GB1286505A - NOVEL PYRIMIDO [5,4-d] PYRIMIDINE DERIVATIVES - Google Patents

Abstract

1286505 Pyrimido[5,4-d]pyrimidine derivatives YAMANOUCHI PHARMACEUTICAL CO Ltd 20 Nov 1969 [20 Nov 1968 22 Nov 1968 25 Jan 1969] 56943/69 Heading C2C Novel, therapeutic compounds I where R is a N-containing heterocycle, R 1 and R 2 are alkyl or NR 3 R 4 where R 3 and R 4 are H, alkyl, cycloalkyl, aralkyl, hydroxyalkyl, alkylaminoalkyl or together with the adjacent N comprise a heterocycle which may contain a further hetero atom, n is 0 or 1 and R 1 and R 2 are each NB 3 <SP>R</SP> 4 when n is 0, are made by reacting NHR 3 R 4 with 4,8 - R,R - disubstituted - 2 - chloro 6 - chlorosulphonyl-pyrimido-pyrimidines (obtained, e.g. from the corresponding 6-mercapto compounds), optionally via the corresponding 2-chlorocompound III or by reacting 4,8-dichloro-compounds corresponding to I with a heterocyclic amine (used for the preparation of the 2,6-dialkylsulphonyl compounds I; the 4,8-dichlorocompounds are made from the 4,8-di-hydroxy 2,6-dialkylsulphonyl compounds utilizing PCl 5 - POCl 3 ). The following intermediates and starting materials, made by standard methods, are also described:-6-chlorosidphonyl-2-methylsulphonyl - and 2,6-bis- (chlorosulphonyl) -4,8-dipiperidinopyrimido[5,4-d]pyrimidines, 4,8-di-hydroxy- 2,6-bis-(methylthio and methylsulhonyl) -pyrimido- [5,4 - d]pyrimidines and 4,8 - dichloro - 2,6 - bis- (chlorosulpheno)- and 4,8 - dipiperidino - 2,6 - bis- (piperidinosulpheno) - pyrimido[5,4 - d]pyrimidines.