Lin-hua Zhang

Pictet-Spengler reaction in trifluoroacetic acid. Large scale synthesis of pyridoindolobenzodiazepine as an atypical antipsychotic agent

Abstract Traditional syntheses of benzodiazepines involve a Bischler-Napieralski reaction which is a three step process and gives low overall yields. An attractive alternative is to construct the diazepine ring under Pictet-Spengler conditions. This paper reports the synthesis of a novel pyridoindolo-benzodiazepine as a potent atypical antipsychotic agent. The key step in the synthesis is the ring formation of the diazepine ring in neat trifluoroacetic acid.

The chiral specific synthesis of DMP 754, a platelet GP IIbIIIa antagonist

Abstract An effective and chiral specific synthesis of DMP 754 ( 1 ), a non-peptide platelet GP IIb IIIa antagonist, is reported.

Facile detosylation of cyclic peptides. An effective synthesis of platelet glycoprotein IIb/IIIa inhibitors

Abstract A general and effective synthesis of cyclic pentapeptides containing Arg-Gly-Asp sequence, which are potent antithrombotic agents, is reported.

Reversal of the regioselectivity of anthrapyrazole formation. A new synthesis of losoxantrone (DUP941)

Losoxantrone, a potent anticancer agent, has been efficiently synthesized in a 6 step process from 5-hydroxy-1,4-dichloroanthracene-9,10-dione.