1338650-07-9

Upstream product

• 367258-59-1 4-(4-bromobenzenesulfonyloxy)-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester 
• 1338650-03-5 tert-butyl (2S,4S)-4-{[(4-bromophenyl)sulfonyl]oxy}-2-{[(1R,2S)-2-ethenyl-1-(ethoxycarbonyl)cyclopropyl]carbamoyl}pyrrolidine-1-carboxylate 
• 1338650-23-9 2-cyclopentyloxycarbonylamino-3-[(2-nitro-benzenesulfonyl)-pent-4-enyl-amino]propionic acid 
• 1338650-04-6 1-{[4-(4-bromobenzenesulfonyloxy)pyrrolidine-2-carbonyl]amino}-2-vinyl-cyclopropane-carboxylic acid ethyl ester hydrogen chloride 
• 635714-19-1 methyl (2S)-2-[(tert-butoxycarbonyl)amino]-3-{[(2-nitrophenyl)sulfonyl]amino}propanoate 
• 790305-06-5 2-tert-butoxycarbonylamino-3-[(2-nitro-benzenesulfonyl)-pent-4-enyl-amino]propionic acid methyl ester 
• 1338649-92-5 2-amino-3-[(2-nitro-benzenesulfonyl)-pent-4-enylamino]propionic acid methyl ester 
• 1338649-93-6 2-cyclopentyloxycarbonylamino-3-[(2-nitro-benzenesulfonyl)-pent-4-enyl-amino]propionic acid methyl ester 
• 138-36-3 p-bromobenzene sulfonic acid 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 1694-92-4 2-Nitrobenzenesulfonyl chloride 

Relevant academic research and scientific papers

A concise synthesis of the HCV protease inhibitor BILN 2061 and its P3 modified analogs

A concise synthesis of BILN 2061 was achieved through more efficient installation of P2 4-quinoline moiety via SN2 displacement of the β-OBs group located on the 4-hydroxyl proline intermediate, which was prepared from 4-α-hydroxyl proline analog via Mitsunobu reaction with inversion of stereochemistry. In addition, a short and practical synthesis for P3 unit is also described herein. Final assembly of four fragments for BILN 2061 was achieved with an overall yield of 58% in 4 steps from P1 to 15a. Furthermore several analogs of BILN 2061 (WX-1-WX-5) containing modifications on P3 unit were synthesized successfully using the same synthetic route as described for the parent inhibitor BILN 2061. Copyright