| 摘要 |
<p>1307590 4 - { 1 - (# - Benzoylalkyl) - 3 - pyrrolidinyl} - 2H - 1,4 - benzoxazin - 3(4H) - ones A H ROBINS CO Inc 3 July 1970 [7 July 1969] 32427/70 Heading C2C Novel 4 - { 1 - (# - benzoylalkyl) - 3 - pyrrolidinyl} - 2H - 1,4 - benzoxazin - 3(4H) - ones of the general formula wherein R is a hydrogen, fluorine, chlorine or bromine atom or a C 1-8 alkyl or C 1-8 alkoxy group and n is 2; 3 or 4, and pharmaceutically acceptable acid addition salts thereof are prepared (a) by condensation of an #-benzoylalkyi halide of the general formula or a cyclic ketal thereof with 4-(3-pyrrolidinyl)- 2H-1,4-benzoxazin-3(4H)-one of the general formula followed, when a cyclic ketal is used, by mild acid hydrolysis and (b) when n is 2, by condensation of an N,N-dialkyl-2-benzoylethyl-. amine of the general formula with 4 - (3 - pyrrolidinyl) - 2H - 1,4 - benzoxazin- 3(4H)-one of the third general formula above, followed optionally by salification of the product. Pharmaceutical compositions having tranquillizing activity comprise, as active ingredient, a 4 - {1 - ( # - benzoylalkyl) - 3 - pyrrolidinyl}- 2H-1,4-benzoxazin-3(4H)-one of the first general formula above or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutically acceptable carrier.</p> |
