Process for preparing 1,5-benzothiazepine derivatives

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

1992-11-19

1994-03-15

Bond, Robert T.

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

Organic compounds

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

C07D28110

Patent

active

052947068

ABSTRACT:
There is disclosed a process for preparing 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, or a salt thereof which comprises subjecting a propionate derivatives of the formula: ##STR2## wherein R.sup.2 is an ester residue and R.sup.1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula:

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Kugita et al, "Synthesis of 1,5-Benzothiazepine Derivatives, I", Chem. Pharm. Bull., 18, 2028-2037 (1970).
Registry of Toxic Effects of Chemical Substances 1985-1986, pp 804 and 5121.
Handbook of Industrial Toxicology, pp. 124-127.

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