HRP20150616T1 - Postupci za pripremu spoja prolijeka inhibitora vezanja hiv-a i intermedijera - Google Patents
Postupci za pripremu spoja prolijeka inhibitora vezanja hiv-a i intermedijera Download PDFInfo
- Publication number
- HRP20150616T1 HRP20150616T1 HRP20150616TT HRP20150616T HRP20150616T1 HR P20150616 T1 HRP20150616 T1 HR P20150616T1 HR P20150616T T HRP20150616T T HR P20150616TT HR P20150616 T HRP20150616 T HR P20150616T HR P20150616 T1 HRP20150616 T1 HR P20150616T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- image
- produce
- conversion
- reaction
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (18)
1. Postupak za pripremu spoja formule I:
[image]
koji sadrži:
(a) brominaciju spoja
[image]
da se proizvede spoj
[image]
i
(b) nitraciju spoja 2 da se proizvede spoj
[image]
i
(c) konverziju amino grupe na spoju 3 u metoksi grupu da se proizvede spoj
[image]
i
(d) zatim konverziju spoja 4 u spoj
[image]
i
(e) konverziju spoja 5 u spoj
[image]
i
(f) formiranje biciklične strukture od spoja 6 da se proizvede
[image]
i
(g) zatim klorinaciju spoja 7 da se proizvede
[image]
i
(h) nakon toga dodavanje triazolil grupe spoju 8 da se proizvede
[image]
i
(i) konverziju spoja 9 do strukture
[image]
i
(j) modifikaciju spoja 10 da se proizvede spoj
[image]
i
(k) reakciju spoja 11 da se proizvede spoj
[image]
i
(l) zatim konverziju spoja 12 u spoj
[image]
(m) zatim konverziju spoja 13 u spoj
[image]
i
(n) zatim reakciju spoja 14 da se proizvede spoj
[image]
i
(o) zatim konverziju spoja 15 do spoja formule I.
2. Postupak za pripremu spoja formule I:
[image]
koji sadrži:
(i) reakciju spoja
[image]
sa
[image]
u prisustvu TMG, NMP i NaI ili K2CO3 i MeCN da se proizvede spoj
[image]
i
(ii) reakciju spoja 11 sa
[image]
da se proizvede spoj
[image]
i
(iii) zatim konverziju spoja 12 do spoja
[image]
(iv) zatim konverziju spoja 13 do spoja
[image]
i
(v) zatim reakciju spoja 14 da se proizvede spoj
[image]
i
(vi) zatim konverziju spoja 15 do spoja formule I.
3. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (a) izveden uporabom Ac2O.
4. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (b) izveden pod kiselim uvjetima.
5. Postupak prema patentnom zahtjevu 4, naznačen time što je korak (b) izveden uporabom dušične kiseline.
6. Postupak prema patentnom zahtjevu 5, naznačen time što je korak (b) izveden uporabom dušične kiseline i sumporne kiseline.
7. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (c) izveden uporabom NaNO2 i TMS-Cl u alkoholu.
8. Postupak prema patentnom zahtjevu 7, naznačen time što je navedeni alkohol metanol.
9. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (d) izveden uporabom
[image]
10. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (h) izveden uporabom
[image]
11. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (i) izveden uporabom
[image]
12. Postupak prema patentnom zahtjevu 1, naznačen time što je korak (j) izveden uporabom
[image]
13. Postupak prema patentnom zahtjevu 2, naznačen time što je korak (ii) izveden uporabom
[image]
14. Postupak prema patentnom zahtjevu 2, naznačen time što je korak (iv) izveden uporabom diklorometana.
15. Postupak prema patentnom zahtjevu 2, naznačen time što je korak (v) izveden uporabom
[image]
16. Postupak prema patentnom zahtjevu 2, naznačen time što je korak (vi) izveden uporabom acetona u vodi i trometaminu.
17. Postupak za pripremu spoja formule (14):
[image]
koji sadrži:
(i) reakciju spoja
[image]
sa
[image]
da se proizvede spoj
[image]
i
(ii) reakciju spoja 11 sa
[image]
da se proizvede spoj
[image]
i
(iii) zatim konverziju spoja 12 u spoj
[image]
uporabom plina klora;
(iv) zatim proizvodnju spoja 14 uporabom diklorometana
[image]
18. Spoj koji ima slijedeću formulu:
[image]
[image]
[image]
ili
[image]
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161437821P | 2011-01-31 | 2011-01-31 | |
| PCT/US2012/022851 WO2012106189A1 (en) | 2011-01-31 | 2012-01-27 | Methods of making hiv attachment inhibitor prodrug compound and intermediates |
| EP20120704960 EP2670751B1 (en) | 2011-01-31 | 2012-01-27 | Methods of making hiv attachment inhibitor prodrug compound and intermediates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20150616T1 true HRP20150616T1 (hr) | 2015-07-03 |
Family
ID=45688987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20150616TT HRP20150616T1 (hr) | 2011-01-31 | 2012-01-27 | Postupci za pripremu spoja prolijeka inhibitora vezanja hiv-a i intermedijera |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8436168B2 (hr) |
| EP (1) | EP2670751B1 (hr) |
| JP (1) | JP6006236B2 (hr) |
| KR (1) | KR101848533B1 (hr) |
| CN (1) | CN103339130B (hr) |
| AR (1) | AR085052A1 (hr) |
| AU (1) | AU2012212508B2 (hr) |
| BR (1) | BR112013018159A2 (hr) |
| CA (1) | CA2826260C (hr) |
| CY (1) | CY1116505T1 (hr) |
| DK (1) | DK2670751T3 (hr) |
| EA (1) | EA021726B1 (hr) |
| ES (1) | ES2539908T3 (hr) |
| HR (1) | HRP20150616T1 (hr) |
| HU (1) | HUE026880T2 (hr) |
| IL (1) | IL227302A (hr) |
| MX (1) | MX2013008371A (hr) |
| PL (1) | PL2670751T3 (hr) |
| PT (1) | PT2670751E (hr) |
| RS (1) | RS54055B1 (hr) |
| SG (1) | SG191841A1 (hr) |
| SI (1) | SI2670751T1 (hr) |
| SM (1) | SMT201500169B (hr) |
| TW (1) | TW201309692A (hr) |
| WO (1) | WO2012106189A1 (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| WO2010085456A1 (en) | 2009-01-20 | 2010-07-29 | Guided Delivery Systems Inc. | Anchor deployment devices and related methods |
| JP6114314B2 (ja) | 2012-02-08 | 2017-04-12 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ付着阻害剤であるピペラジンプロドラッグ化合物の製造方法 |
| CN106575528B (zh) * | 2014-06-23 | 2019-08-23 | 自由形态纤维有限公司 | 用于核反应堆燃料的加工和特征描述的增材制造技术 |
| KR20170096021A (ko) | 2014-12-18 | 2017-08-23 | 비브 헬스케어 유케이 (넘버4) 리미티드 | 보록신을 사용하여 할로겐화된 아자인돌 화합물을 제조하는 방법 |
| CA2971096A1 (en) | 2014-12-18 | 2016-06-23 | ViiV Healthcare UK (No.4) Limited | A process for preparing halogenated azaindole compounds using pybrop |
| EP4292551A3 (en) | 2015-03-05 | 2024-01-31 | Ancora Heart, Inc. | Devices of visualizing and determining depth of penetration in cardiac tissue |
| ES2972293T3 (es) | 2019-01-17 | 2024-06-12 | Viiv Healthcare Uk No 4 Ltd | Procedimiento para preparar fostemsavir |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| US7776863B2 (en) | 2004-03-24 | 2010-08-17 | Bristol-Myers Squibb Company | Methods of treating HIV infection |
| US7601715B2 (en) | 2005-06-22 | 2009-10-13 | Bristol-Myers Squibb Company | Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein |
| US7851476B2 (en) * | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
-
2012
- 2012-01-27 HR HRP20150616TT patent/HRP20150616T1/hr unknown
- 2012-01-27 ES ES12704960.9T patent/ES2539908T3/es active Active
- 2012-01-27 BR BR112013018159A patent/BR112013018159A2/pt not_active Application Discontinuation
- 2012-01-27 WO PCT/US2012/022851 patent/WO2012106189A1/en active Application Filing
- 2012-01-27 PT PT127049609T patent/PT2670751E/pt unknown
- 2012-01-27 SG SG2013051560A patent/SG191841A1/en unknown
- 2012-01-27 KR KR1020137022709A patent/KR101848533B1/ko active Active
- 2012-01-27 DK DK12704960.9T patent/DK2670751T3/en active
- 2012-01-27 SI SI201230225T patent/SI2670751T1/sl unknown
- 2012-01-27 RS RS20150388A patent/RS54055B1/en unknown
- 2012-01-27 MX MX2013008371A patent/MX2013008371A/es active IP Right Grant
- 2012-01-27 JP JP2013551361A patent/JP6006236B2/ja active Active
- 2012-01-27 EP EP20120704960 patent/EP2670751B1/en active Active
- 2012-01-27 CA CA2826260A patent/CA2826260C/en not_active Expired - Fee Related
- 2012-01-27 CN CN201280007153.8A patent/CN103339130B/zh not_active Expired - Fee Related
- 2012-01-27 HU HUE12704960A patent/HUE026880T2/en unknown
- 2012-01-27 PL PL12704960T patent/PL2670751T3/pl unknown
- 2012-01-27 US US13/359,708 patent/US8436168B2/en active Active
- 2012-01-27 EA EA201391123A patent/EA021726B1/ru not_active IP Right Cessation
- 2012-01-27 AU AU2012212508A patent/AU2012212508B2/en not_active Ceased
- 2012-01-31 TW TW101103123A patent/TW201309692A/zh unknown
- 2012-01-31 AR ARP120100313A patent/AR085052A1/es not_active Application Discontinuation
-
2013
- 2013-07-02 IL IL227302A patent/IL227302A/en active IP Right Grant
-
2015
- 2015-07-14 SM SM201500169T patent/SMT201500169B/xx unknown
- 2015-07-17 CY CY20151100631T patent/CY1116505T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL2670751T3 (pl) | 2015-09-30 |
| PT2670751E (pt) | 2015-07-29 |
| SI2670751T1 (sl) | 2015-07-31 |
| EA021726B1 (ru) | 2015-08-31 |
| EA201391123A1 (ru) | 2013-12-30 |
| RS54055B1 (en) | 2015-10-30 |
| SG191841A1 (en) | 2013-08-30 |
| BR112013018159A2 (pt) | 2018-09-11 |
| JP2014503594A (ja) | 2014-02-13 |
| TW201309692A (zh) | 2013-03-01 |
| US20130030178A1 (en) | 2013-01-31 |
| MX2013008371A (es) | 2013-08-12 |
| KR101848533B1 (ko) | 2018-04-12 |
| DK2670751T3 (en) | 2015-07-20 |
| WO2012106189A1 (en) | 2012-08-09 |
| IL227302A0 (en) | 2013-09-30 |
| AU2012212508B2 (en) | 2016-01-14 |
| AR085052A1 (es) | 2013-08-07 |
| KR20140014154A (ko) | 2014-02-05 |
| CN103339130A (zh) | 2013-10-02 |
| SMT201500169B (it) | 2015-09-07 |
| CA2826260A1 (en) | 2012-08-09 |
| EP2670751A1 (en) | 2013-12-11 |
| AU2012212508A1 (en) | 2013-09-19 |
| CY1116505T1 (el) | 2017-03-15 |
| US8436168B2 (en) | 2013-05-07 |
| CN103339130B (zh) | 2015-05-06 |
| EP2670751B1 (en) | 2015-04-22 |
| ES2539908T3 (es) | 2015-07-07 |
| IL227302A (en) | 2016-10-31 |
| JP6006236B2 (ja) | 2016-10-12 |
| HUE026880T2 (en) | 2016-08-29 |
| CA2826260C (en) | 2018-09-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20150616T1 (hr) | Postupci za pripremu spoja prolijeka inhibitora vezanja hiv-a i intermedijera | |
| MX2013011257A (es) | Proceso para la preparacion de dronedarona por n-butilacion. | |
| MY148612A (en) | Process for preparation of high purity methacrylic acid | |
| HRP20160241T1 (hr) | Postupci i intermedijeri za pripravu jak inhibitora | |
| MX2013011259A (es) | Proceso de aminacion reductora para la preparacion de la dronedarona usando el compuesto intermediario de amina. | |
| WO2012009699A3 (en) | Process for preparing antiviral compounds | |
| WO2009017091A1 (ja) | β－ニトロスチレン化合物の製造方法 | |
| TR201905687T4 (tr) | Travoprost hazırlanışına yönelik proses. | |
| JP2016520038A5 (hr) | ||
| WO2011015287A3 (en) | Process for the preparation of derivatives of 1-(2-halobiphenyl-4-yl)-cyclopropanecarboxylic acid | |
| IN2014DN00144A (hr) | ||
| EP2452931A4 (en) | PROCESS FOR THE PREPARATION OF TRICYCLIC DERIVATIVES | |
| UA111868C2 (uk) | Спосіб одержання естерів (5-фтор-2-метил-3-хінолін-2-ілметиліндол-1-іл)-оцтової кислоти | |
| NZ577081A (en) | Synthesis of compounds useful as modulators of amyloid-beta production | |
| MY161504A (en) | Process for preparation of methacrylic acid and methacrylic acid esters | |
| HRP20170379T1 (hr) | Postupak proizvodnje naltreksona | |
| UA104684C2 (ru) | Промежуточное соединение для получения агомелатина (варианты) и способ его получения (варианты) | |
| WO2012164242A8 (en) | Process for the preparation of paliperidone | |
| WO2012044043A3 (en) | Novel method of preparing benzoimidazole derivatives | |
| CU24311B1 (es) | Método de preparación de compuestos alfa-galactosil ceramidas | |
| HRP20192143T1 (hr) | Postupak za pripravu 1-(3,5-diklorofenil)-2,2,2-trifluoroetanona i njegovih derivata | |
| CN102531897A (zh) | 一种制备α-取代丙二酸二乙酯衍生物的方法 | |
| UY33342A (es) | Proceso para la preparación de amidas de ácido pirazol carboxílico | |
| MX2013004193A (es) | Procedimiento para la preparacion de derivados de acido 3-(6-amino-piridin-3-il)-2-acrilico. | |
| MY165642A (en) | Process for preparation of methacrylic acid and methacrylic acid ester |