method for preparation of medicines with anti serotonin, anti histamine, antiemetic and analgesic effect, the formed productand the preparation of the medicines to use active compounds.

摘要

1,242,096. Benzo[b]benzofurano[2,3 - e]- oxepines. LABAZ. 3 Dec., 1969 [20 Dec., 1968], No. 60855/68. Heading C2C. Novel benzo[b]benzofurano[2,3-e]oxepines of the general formula wherein R 1 is a #-dimethylaminoethyl, #-dimethylaminoisopropyl, #-piperidinoethyl, #-(4- methylpiperazino)ethyl, (1 - methyl - 2 - piperidyl) - methyl or 1 - methyl - 3 - piperidyl group, R 2 is a hydrogen atom or methyl group, R 3 is a hydrogen or chlorine atom or a methyl or methoxy group, R 4 is a hydrogen atom or methyl group and R 5 is a hydrogen or chlorine atom or a methoxy group, and pharmaceutically acceptable acid addition salts thereof are prepared by reaction of a 6-hydroxybenzo[6]- benzofurano[2,3-e]oxepine of the general formula with a dehydrating agent, followed optionally by salification of the product. 6 - Hydroxy - benzo [b] benzofurano [2,3 - e]- oxepines of the second general formula above are prepared by reaction of an ethyl 3-bromomethyl-coumarilate and a phenol of the respective general formulµ followed by saponification, treatment of the resulting 3 - phenoxymethyl - coumarilic acid of the general formula with thionyl chloride, followed by cyclization and reaction of the resulting 6-oxo-benzo[b]- benzofurano[2,3-e]oxepine of the general formula with a Grignard reagent of the general formula HalMg-CH 2 -R 1 , wherein Hal is a chlorine or bromine atom, followed by hydrolysis. Pharmaceutical compositions having serotonin- and histamine-antagonistic, antalgic and antiemetic activity comprise, as active ingredient, a benzo[b]benzofurano[2,3-e]oxepine of the first general formula above or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutical carrier, and may be administered orally, rectally or parenterally.