| 摘要 |
The present invention relates to a process for preparation of amino substituted benzothiazole derivatives of formula I wherein R<1>, R<2 >and R<3 >are independently from each other hydrogen, lower alkyl, lower alkoxy or halogen; R<4 >is hydrogen, lower alkyl, lower alkyloxy, halogen, or is a five or six membered non aromatic heterocyclyl group, unsubstituted or substituted by lower alkyl or an oxo-group, or is -NR<5>R<6>, wherein R<5 >and R<5 >are independently from each other hydrogen, lower alkyl, -C(O)-lower alkyl, -(CH2)nO-lower alkyl or benzyl, opionally substituted by lower alkyl, or is an five or six membered heteroaryl group; R<1 >and R<2 >or R<2 >and R<3 >may form together with the corresponding carbon atoms a ring containing -O-CH2-O- or -CH=CH-CH=CH-; R is hydrogen or -C(O)R'; R' is a five or six membered non aromatic heterocyclyl group, five or six membered heteroaryl group or is aryl, which rings may be substituted by the groups, selected from lower alkyl, halogen-lower alkyl, lower alkoxy, cyano, nitro, -C(O)H, -C(O)OH or by pyrrolidin-1-yl-methyl; n is 1 to 4; or a pharmaceutically acceptable salt thereof, wherein the cyclization is carried out by the treatment of a compound of formula with sulphoxide/HBr/solvent to give the desired products of formula I for R is hydrogen (formula IA) or for R is -C(O)R' (formula IB)
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