pHarmacist (Hive Bee) 11-15-02 18:51 No 380034				Synthesis of benzodiazepines	Bookmark
						Patent US5466799 Abstract A general method is provided for the synthesis of substituted 2,3-dihydro-5-phenyl-1H-1,4-benzodiazepines by the reaction of bis-trifiated-2,5-dihydroxy benzophenones with 1,2-bisaminoethanes, followed by displacement of the 7-trifloxy group. ... ...Although 5-phenyl-3H-1,4-benzodiazepin-2-(1H)-one can be prepared from 2-aminobenzophenone and glycine ether ester hydrochloride in one step, the synthesis of ring-substituted benzodiazepines requires the use of bis-substituted benzophenones, such as 2-amino-5-chlorobenzophenone, that are both more difficult to obtain and to manipulate. See, for example, U.S. Pat. No. 3,313,815. Thus, a need exists for new syntheses of benzodiazepines that can be readily adapted to the synthesis of a variety of known and novel diazepam analogs... Dedicated to weedar There Can Only Bee One - xX www.the-hive.ws Xx
		SPISSHAK (Hive Bee) 11-16-02 23:58 No 380331				Pharmacist	Bookmark
						I happen to be in pharmacy scholl myself. But if yu look under the klonazepam synthesis on rhodium's page you will find a preaparation of a 5-nitro, -2- chloro amino benzophenone. Via a Freidel crafts reaction between 2-chloro benzoyl choride, and a 4-nitroanaline. using ZnCl2 as a Lewis acid catalyst. the yeilds are low I suspect because of side reactions like the formation of an anilide, and multiple frediel crafts alkyltions. but it's there. I have a question once you have the bromacetamido chloro, nitro benzophenone, and you react it with hexamethylene tertamine in the presecne of an acid; what is the cycliization mechanism that produces your benzdazopinone? Cyclization mechanisms can be tricky to decipher.
		Rhodium (Chief Bee) 11-17-02 00:19 No 380337				HMTA cyclization	Bookmark
						Spisshak: It might be found in ../rhodium/pdf /benzodiazepine.chemistry.review.pdf