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CAPLUS COPYRIGHT 2012 ACS
||Process for preparation of benzoylaminobenzoylbenzazepinones by reaction of benzazepinones with benzoylaminophenyl halides in the presence of carbonylating agents.
||Torisawa, Yasuhiro; Abe, Kaoru; Muguruma, Yasuaki; Fujita, Shigekazu; Ogawa, Hidenori; Utsumi, Naoto; Miyake, Masahiro
||Otsuka Pharmaceutical Co., Ltd., Japan
||PCT Int. Appl., 44pp. CODEN: PIXXD2
The Title compds. (I; X1 = halo; R1, R2 = alkyl) were prepared by reaction of benzazepinones (II; X1 as above) with halides (III; R1, R2 as above; X2 = halo) in the presence of a carbonylating agent. Thus, a mixture of 2-bromo-5-(2-methylbenzoylamino)toluene (preparation given), 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one, DBU, Ph3P, and Pd(OAc)2 in DMF was heated under CO at 125ｰ for 3 h to give 85% 7-chloro-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one of 99.1% purity.
View the full-text USPTO patent here.
Note: Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the U.S. granted patent is Process for preparing bezazepine compounds or salts thereof. For the CAplus record, this title was enhanced to read Process for preparation of benzoylaminobenzoylbenzazepinones by reaction of benzazepinones with benzoylaminophenyl halides in the presence of carbonylating agents.