Process for preparing 1,5-benzothiazepine derivatives

Details Process for preparing 1,5-benzothiazepine derivatives Process for preparing 1,5-benzothiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/238.6

C07D 281/10 (2006.01) A61K 31/55 (2006.01) C07D 281/00 (2006.01) C07D 281/02 (2006.01)

Patent

CA 1312077

Abstract: Process for preparing 1,5-benzothiazepine derivatives There is disclosed a process for preparing 1,5-benzothiaze- pine derivatives represented by the formula: Image (I) wherein R1 is a lower alkyl group or a lower alkoxy group, R2 is hydrogen or a lower alkanoyl group, one of R3 and R4 is a lower alkyl group or halogen atom, and the other is hydrogen, and each of R5 and R6 is a lower alkyl group, or a pharmaceutically acceptable acid addition salt thereof, which comprises reacting a compound represented by the formula: Image (II) wherein R1, R2, R3 and R4 have the same meanings as defined above, with an aminoethanol represented by the formula: Image (III) wherein R5 and R6 have the same meanings as defined above, and Z is hydrogen, a lower alkylsulfonyl group, an arylsulfonyl group or sulfo group, to condensation reaction and, if necessary, convert it to a pharmaceutacally acceptable acid addition salt thereof.

571434

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