GB1210520A - Glycine derivatives and a process for the preparation thereof - Google Patents

Abstract

1,210,520. 2,2,2-Trihaloethyl glycinates. BRISTOL-MYERS CO. 28 Dec., 1967 [28 Dec., 1966], No. 58905/67. Heading C2C. Novel 2,2,2-trihaloethyl glycinates of the general formula X 3 C-CH 2 -O 2 C-CH 2 -NH 2 , wherein X is chloro or bromo, and pharmaceutically acceptable, non-toxic acid addition salts thereof are prepared by acylation of a 2,2,2-trihaloethanol of the general formula with an acetic acid derivative of the general formula HOOC-CH 2 -Z, wherein Z is amino, chloro, bromo or iodo, or with a reactive functional derivative thereof and, when Z is chloro, bromo or iodo, subsequent treatment with liquid ammonia or concentrated ammonium hydroxide solution, followed by optional conversion of the product to a pharmaceutically acceptable, non- toxic acid addition salt thereof. Pharmaceutical compositions having sedative, hypnotic and anaesthetic activity comprise, as active ingredient, a 2,2,2-trihaloethyl glycinate of the first general formula above or a pharmaceutically acceptable, non-toxic acid addition salt thereof, together with a diluent or carrier, and may be administered orally, parenterally or rectally.