BR9814266A - Processo para a preparação de oxazafosforin-2-aminas - Google Patents
Processo para a preparação de oxazafosforin-2-aminasInfo
- Publication number
- BR9814266A BR9814266A BR9814266-6A BR9814266A BR9814266A BR 9814266 A BR9814266 A BR 9814266A BR 9814266 A BR9814266 A BR 9814266A BR 9814266 A BR9814266 A BR 9814266A
- Authority
- BR
- Brazil
- Prior art keywords
- represent
- chlorethyl
- phenylethyl
- oxazafosforin
- amines
- Prior art date
Links
Classifications
-
- 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
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
- C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
- C07F9/65842—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
- C07F9/65846—Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Transplantation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Patente de Invenção: <B>"PROCESSO PARA A PREPARAçãO DE OXAZAFOSFORIN-2-AMINAS"<D>. A presente invenção refere-se a um método para preparar oxazafosforin-2-aminas da fórmula geral (1), na qual R~ 1~ pode representar H, 2-brometila, 2-cloretila, 2-hidroxietila, 2-mesiloxietila ou 1-feniletila, R~ 2~ pode representar H ou 2-cloretila, R~ 3~ pode representar H, 2-brometila, 2-cloretila ou 1-feniletila e R~ 4~ pode representar H, R~ 1~ e R~ 2~ bem como R~ 3~ e R~ 4~ também podem formar juntos com o átomo de N ligado a um composto aziridina cíclico com a condição de que R~ 1~, R~ 2~ e R~ 3~ não podem representar juntos H e que R~ 1~ e R~ 3~ não podem representar simultaneamente 1-feniletila. Y representa cloreto de hidrogênio ou brometo ou nada. Os compostos obtidos usando este novo método são conhecidos medicamentos tais como ciclofosfamida e ifosfamida que são aplicados como citostáticos ou agentes imunossupressores. As aminas (2) e (3) aplicadas como compostos de partida são reagidas durante uma reação de uma etapa com cloreto de fosforila e com uma base adicional usada como agente fixador de ácidos tal como piridina, trietilamina ou carbonatos de metal alcalino ou de metal alcalino-terroso. A reação é efetuada na presença de solventes inertes enquanto reduz-se ao mínimo a influência da água e sem isolamento de um composto intermediário.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19739159A DE19739159C1 (de) | 1997-09-06 | 1997-09-06 | Verfahren zur Herstellung von Oxazaphosphorin-2-aminen |
| PCT/EP1998/005170 WO1999012942A1 (de) | 1997-09-06 | 1998-08-14 | Verfahren zur herstellung von oxazaphosphorin-2-aminen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR9814266A true BR9814266A (pt) | 2001-10-09 |
| BR9814266B1 BR9814266B1 (pt) | 2009-05-05 |
Family
ID=7841505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI9814266-6A BR9814266B1 (pt) | 1997-09-06 | 1998-08-14 | processo para a preparação de oxazafosforin-2-aminas. |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6187941B1 (pt) |
| EP (1) | EP1012152B1 (pt) |
| JP (1) | JP4278859B2 (pt) |
| CN (1) | CN1147498C (pt) |
| AR (1) | AR013467A1 (pt) |
| AT (1) | ATE225797T1 (pt) |
| BR (1) | BR9814266B1 (pt) |
| CA (1) | CA2301104C (pt) |
| DE (2) | DE19739159C1 (pt) |
| DK (1) | DK1012152T3 (pt) |
| ES (1) | ES2185220T3 (pt) |
| HK (1) | HK1030422A1 (pt) |
| HU (1) | HU226887B1 (pt) |
| IL (1) | IL134507A (pt) |
| IN (1) | IN186170B (pt) |
| PL (1) | PL190097B1 (pt) |
| PT (1) | PT1012152E (pt) |
| WO (1) | WO1999012942A1 (pt) |
| ZA (1) | ZA987741B (pt) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1607204B (zh) * | 2003-10-13 | 2011-10-26 | 北京大学 | 环磷酰胺季铵盐衍生物及其合成和应用 |
| US20110054081A1 (en) * | 2009-09-02 | 2011-03-03 | Frank Dierschke | Formulation and its use |
| FR2968662B1 (fr) * | 2010-12-10 | 2013-11-22 | Roussy Inst Gustave | Nouveaux derives d'oxazaphosphorines pre-activees, utilisation et methode de preparation |
| US20180086780A1 (en) | 2015-04-02 | 2018-03-29 | Przedsiebiorstwo Produkcyjno-Wdrozeniowe Ifotam Sp. Z O.O. | Method of production of n,n-bis(2-chloroethyl)tetrahydro-2h-1,3,2-oxazaphosphorine-2-amine 2-oxide |
| CN107936061B (zh) * | 2017-12-28 | 2019-08-06 | 山东铂源药业有限公司 | 一种环磷酰胺的合成方法 |
| CN109535201B (zh) * | 2019-01-25 | 2020-04-03 | 连云港贵科药业有限公司 | 一种环磷酰胺的合成方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE563332A (pt) * | 1956-12-20 | |||
| US3732340A (en) * | 1966-07-11 | 1973-05-08 | Asta Werke Ag Chem Fab | N',o-propylene phosphoric acid ester diamides |
| DE1645921C3 (de) * | 1966-07-11 | 1978-10-12 | Asta-Werke Ag Chemische Fabrik, 4800 Bielefeld | 2-Oxo-13,2-osazaphosphorinane, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Präparate |
| GB1235022A (en) * | 1969-06-04 | 1971-06-09 | Laeaeke Ag | A new method for the production of cyclophosphamide |
| JPS54157581A (en) * | 1978-05-29 | 1979-12-12 | Otsuka Pharmaceut Co Ltd | Oxazaphosphorine derivative |
| JPS54157580A (en) * | 1978-05-29 | 1979-12-12 | Otsuka Pharmaceut Co Ltd | Optically active oxazaphosphorine derivative |
| PL119971B1 (en) * | 1978-11-06 | 1982-02-27 | Polska Akad Nauk Centrum | Process for preparing optically active derivatives of 1,3,2-oxazaphosphorinane,2-oksazofosforinata |
| JPS5826919B2 (ja) * | 1978-11-07 | 1983-06-06 | 大塚製薬株式会社 | シクロ↓−１，３，２↓−オキサアザホスホル誘導体の製造法 |
| JPS5931787A (ja) * | 1982-08-13 | 1984-02-20 | Otsuka Pharmaceut Co Ltd | １，３，２−オキサアザホスホリナン−２−オキシド誘導体 |
| PL149593B1 (pl) * | 1986-12-18 | 1990-02-28 | Sposób wytwarzania n-acylowych pochodnych 1 , 3 , 2-oksazafosforinanu |
-
1997
- 1997-09-06 DE DE19739159A patent/DE19739159C1/de not_active Expired - Lifetime
-
1998
- 1998-08-14 PT PT98945245T patent/PT1012152E/pt unknown
- 1998-08-14 IL IL13450798A patent/IL134507A/en not_active IP Right Cessation
- 1998-08-14 ES ES98945245T patent/ES2185220T3/es not_active Expired - Lifetime
- 1998-08-14 DK DK98945245T patent/DK1012152T3/da active
- 1998-08-14 HU HU0003496A patent/HU226887B1/hu not_active IP Right Cessation
- 1998-08-14 CN CNB988087529A patent/CN1147498C/zh not_active Expired - Lifetime
- 1998-08-14 WO PCT/EP1998/005170 patent/WO1999012942A1/de active IP Right Grant
- 1998-08-14 JP JP2000510748A patent/JP4278859B2/ja not_active Expired - Fee Related
- 1998-08-14 DE DE59805920T patent/DE59805920D1/de not_active Expired - Lifetime
- 1998-08-14 PL PL98339188A patent/PL190097B1/pl unknown
- 1998-08-14 CA CA002301104A patent/CA2301104C/en not_active Expired - Fee Related
- 1998-08-14 EP EP98945245A patent/EP1012152B1/de not_active Expired - Lifetime
- 1998-08-14 AT AT98945245T patent/ATE225797T1/de active
- 1998-08-14 BR BRPI9814266-6A patent/BR9814266B1/pt not_active IP Right Cessation
- 1998-08-26 ZA ZA987741A patent/ZA987741B/xx unknown
- 1998-09-01 IN IN1574CA1998 patent/IN186170B/en unknown
- 1998-09-04 AR ARP980104431A patent/AR013467A1/es active IP Right Grant
- 1998-09-08 US US09/149,099 patent/US6187941B1/en not_active Expired - Lifetime
-
2001
- 2001-02-23 HK HK01101318A patent/HK1030422A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| HU226887B1 (en) | 2010-01-28 |
| HUP0003496A2 (hu) | 2002-11-28 |
| DE59805920D1 (de) | 2002-11-14 |
| CA2301104A1 (en) | 1999-03-18 |
| JP4278859B2 (ja) | 2009-06-17 |
| ZA987741B (en) | 1998-10-08 |
| PL339188A1 (en) | 2000-12-04 |
| PL190097B1 (pl) | 2005-10-31 |
| EP1012152B1 (de) | 2002-10-09 |
| DK1012152T3 (da) | 2003-02-10 |
| PT1012152E (pt) | 2003-02-28 |
| ES2185220T3 (es) | 2003-04-16 |
| CA2301104C (en) | 2009-10-20 |
| US6187941B1 (en) | 2001-02-13 |
| JP2001515910A (ja) | 2001-09-25 |
| HK1030422A1 (en) | 2001-05-04 |
| IN186170B (pt) | 2001-06-30 |
| BR9814266B1 (pt) | 2009-05-05 |
| IL134507A0 (en) | 2001-04-30 |
| WO1999012942A1 (de) | 1999-03-18 |
| CN1268950A (zh) | 2000-10-04 |
| HUP0003496A3 (en) | 2002-12-28 |
| ATE225797T1 (de) | 2002-10-15 |
| DE19739159C1 (de) | 1999-01-28 |
| CN1147498C (zh) | 2004-04-28 |
| IL134507A (en) | 2004-06-20 |
| AR013467A1 (es) | 2000-12-27 |
| EP1012152A1 (de) | 2000-06-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B25A | Requested transfer of rights approved |
Owner name: BAXTER INTERNATIONAL INC. (US) , BAXTER HEALTHCARE Free format text: TRANSFERIDO DE: ASTA MEDICA AKTIENGESELLSCHAFT |
|
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 28/07/2009, OBSERVADAS AS CONDICOES LEGAIS. |
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| B25I | Requirement for requested change of headquarter |
Owner name: BAXTER INTERNATIONAL INC. (US) , BAXTER HEALTHCARE Free format text: A FIM DE ATENDER A ALT. DE SEDE REQUERIDA ATRAVES DA PET. NO 020090120869-RJ, DE 28/12/2009, E NECESSARIO COMPLEMENTAR O VALOR DA GUIA CORRESPONDENTE A ESTE ATO, BEM COMO RECOLHER A REFERENTE AO CUMPRIMENTO DESTA EXIGENCIA. |
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| B25I | Requirement for requested change of headquarter |
Owner name: BAXTER INTERNATIONAL INC. (US) , BAXTER HEALTHCARE Free format text: AFIM DE ATENDER A ALTERACAO DE ENDERECO REQUERIDA ATRAVES DA PETICAO NO 020090120869/RJ DE 28/12/2009, E NECESSARIO COMPLETAR O VALOR DA GUIA CORRESPONDENTE, TENDO EM VISTA QUE A COMPLEMENTACAO APRESENTADA NA PETICAO NO 020110064764/RJ DE 20/06/2011, NAO FOI SUFICIENTE PARA ATENDER TODOS OS PEDIDOS RELACIONADOS PARA A ALTERACAO DE ENDERECO. |
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| B25G | Requested change of headquarter approved |
Owner name: BAXTER INTERNATIONAL INC. (US) , BAXTER HEALTHCARE Free format text: ENDERECO DO 2O DEPOSITANTE ALTERADO CONFORME SOLICITADO NA PETICAO NO 020110115944/RJ DE 11/11/2011. |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 21A ANUIDADE. |
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| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2527 DE 11-06-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |