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The Conversion of 2-(2-Chloroacetamido)benzophenones into 2,3-Dihydro-2-oxo-1,4-benzodiazepines. Part III. Further consideration of the hexamine system
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Clarke, George M.,Lee, J. Barry,Swinbourne, Frederick J.,Williamson, Basil
p. 4777 - 4793
(2007/10/02)

Process for the preparation of 1,4-benzodiazepine derivatives
A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, SPC1 Wherein R1 is hydrogen, halogen, nitro or trifluoromethyl; R2 and R3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxyalkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula EQU1 in which R6 and R7 are independently lower alkyl, and n is an integer of 1 to 4; and R5 is hydrogen or lower alkyl, is obtained by reacting a benzophenone derivative of the formula, SPC2 Wherein R1, R2, R3 and R4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula EQU2 wherein R5 is as defined above.
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(2008/06/13)