Process for preparing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzo

Details Process for preparing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzo Process for preparing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzo

1990-11-19

1992-07-07

Bond, Robert T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

C07D30613

Patent

active

051284685

ABSTRACT:
The present invention relates to a novel process for synthetizing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzothiazepin-4(5H)-ones and their derivatives, an optically pure compounds or as their racemic mixtures, having the following general formula (I): ##STR1## by using, as synthesis precursors, methyl esters of 2-hydroxy-3-arylthio-3-arylpropionic acids in their threo form, as their hydrochlorides, or as free bases, of generally formula (II): ##STR2## and treating such precursors with an excess of sodium methoxide, at low temperature, in diethyleneglycol, dimethylether, diemthylformamide and ethyl acetate.

REFERENCES:
patent: 4590188 (1986-03-01), Takeda et al.
patent: 5008411 (1991-04-01), Coffen et al.
patent: 5008433 (1991-01-01), Palmer

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