186431-53-8

Upstream product

• 79-37-8 oxalyl dichloride 
• 204381-53-3 Benzoic acid 1-((S)-2-tert-butoxycarbonylamino-3-phenyl-propionyl)-pyrrolidin-3-yl ester 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 448236-06-4 (R)-N-[N-(tert-butoxycarbonyl)-L-phenylalanyl]pyrrolidin-3-ol 
• 186431-54-9 1-[(tert-butoxycarbonyl)-L-phenylalanyl]-3(R,S)-pyrrolidinol 

Downstream Products

• 204381-60-2 1-((S)-2-Amino-3-phenyl-propionyl)-pyrrolidin-3-one 
• 204381-62-4 N-[N-(quinolin-2-ylcarbonyl)-L-phenylalanyl]pyrrolidin-3-one 
• 204381-63-5 N-(N-nicotinoyl-L-phenylalanyl)pyrrolidin-3-one 

Relevant academic research and scientific papers

Parallel synthesis of new phenylalanino-2-(phenylthio)pyrrolidin-3-one scaffold-based analogues

Based on the specific PhePro proteolytic cleavage of the HIV-protease, we synthesized short pseudopeptides incorporating a 2-(phenylthio)pyrrolidin-3-one ring. We previously described various analogues based on this scaffold. We report herein a parallel m

Process for the preparation of substituted N-(indole-2-carbonyl)- glycinamides

Processes and intermediates for preparing compounds of Formula (I).

Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors

PCT No. PCT/IB95/00442 Sec. 371 Date Dec. 2, 1997 Sec. 102(e) Date Dec. 2, 1997 PCT Filed Jun. 6, 1995 PCT Pub. No. WO96/39384 PCT Pub. Date Dec. 12, 1996Compounds of Formula (1) wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR8R9 or C(O)R12 as glucogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.

Use of proline bioisosteres in potential HIV protease inhibitors: Phenylalanine-2-thiophenoxy-3-pyrrolidinone: Synthesis and anti-HIV evaluation

The synthesis of new phenylalanine-2-thiophenoxy-3-pyrrolidinones is described. Anti-HIV recombinant protease assays and HIV infected cell culture assays (observation of syncytia) demonstrated the potent anti-HIV activity of this new class of pseudopeptides. (C) 2000 Published by Elsevier Science Ltd.

Short and unexpectedly potent 3-pyrrolidinone type inhibitors of HIV-1 replication

Based on the specific PhePro proteolytic cleavage of the HIV protease, short pseudo-peptides incorporating a 3-pyrrolidinone none ring have been synthesized. Their potencies to inhibit HIV-1 in MT4 cell culture have been evaluated and compared to that of the bioisostere dipeptide BocPhePro. Analogues incorporating an aromatic residue have shown to inhibit HIV-1 infection in MT4 human lymphoid cell with an IC50 ranging from 1 to 10 μM. Further experiments are in progress to determine their HIV protease inhibition properties.

Syntheses of new modified Phe-Pro peptides. Use of proline replacements in potential HIV inhibitors

The syntheses consisting of replacement of proline amino acid by a 3-pyrrolidinone ring in Phe-Pro analogues are described. Preliminary anti-HIV studies demonstrated the potential activity of this new class of compounds.