78281-71-7Relevant articles and documents
Development and a practical synthesis of nepafenac intermediate via modified gassman reaction
Cybulski, Marcin,Formela, Adam,Mucha, Mariola,Klos, Karolina,Roszczynski, Jacek,Winiarski, Jerzy
, p. 461 - 464,4 (2020/08/24)
Modification of nepafenac intermediate synthesis (5A) via Gassman specific ortho-substitution is reported. According to the process, 2-aminobenzophenone (1A) and 2-(methylthio)acetamide (2) were reacted in the convenient temperature conditions, in the presence of N-chlorophthalimide (3) or 1,3-dichloro-5,5- dimethylhydantoin (4), to activate the formation of azasulfonium salt and rearrangement thereof to pure 2-amino-3-benzoyl-α-(methylthio) phenylacetamide (5A). The procedure appears to be suitable for a reaction carried out in a large scale.
Method of producing an inhibitory effect on blood platelet aggregation
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, (2008/06/13)
Novel 2-amino-3-benzoyl-phenylacetamides are provided having the formula: STR1 wherein R represents hydrogen or lower alkyl, R1 and R2 represent hydrogen, lower alkyl, cycloalkyl, phenyl and phenyl substituted by lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl, and R1 and R2 when taken together with the adjacent nitrogen may form a heterocyclic residue; X represents hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; Y represents hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, lower alkylthio, lower alkyloxythio or lower alkyldioxythio; Am is primary amino (--NH2), methylamino or dimethylamino, and n is 1 to 3 inclusive. The compounds exhibit anti-inflammatory, antipyretic, anti-blood platelet aggregation and analgetic pharmacological activities.