367258-59-1

Upstream product

• 438452-29-0 1-tert-butyl 2-methyl (2S,4S)-4-{[(4-bromo-phenyl)sulfonyl]oxy}-pyrrolidine-1,2-dicarboxylate 
• 138-36-3 p-bromobenzene sulfonic acid 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 

Downstream Products

• 874124-85-3 C₂₅H₃₂BrN₃O₉S₂ 
• 1219513-73-1 C₂₃H₃₁BrN₂O₈S 
• 1338650-03-5 tert-butyl (2S,4S)-4-{[(4-bromophenyl)sulfonyl]oxy}-2-{[(1R,2S)-2-ethenyl-1-(ethoxycarbonyl)cyclopropyl]carbamoyl}pyrrolidine-1-carboxylate 
• 769167-58-0 (1S,2R)-1-{[(2S,4S)-4-(4-bromo-benzenesulfonyloxy)-1-((S)-2-cyclopentyloxycarbonylamino-oct-7-enoyl)pyrrolidine-2-carbonyl]-amino}-2-vinylcyclopropanecarboxylic acid methyl ester 
• 879623-40-2 18-(4-bromobenzenesulfonyloxy)-14-cyclopentyloxycarbonylamino-2,15-dioxo-3,16-diaza-tricyclo-[14.3.0.0(4,6)]nonadec-7-ene-4-carboxylic acid methyl ester 
• 1098199-68-8 C₁₈H₂₁BrN₂O₆S*ClH 
• 1338650-04-6 1-{[4-(4-bromobenzenesulfonyloxy)pyrrolidine-2-carbonyl]amino}-2-vinyl-cyclopropane-carboxylic acid ethyl ester hydrogen chloride 
• 1007205-38-0 ciluprevir 
• 1338650-05-7 1-{[4-(4-bromobenzenesulfonyloxy)-1-(2-cyclopentyloxycarbonylamino-3-pent-4-enyloxypropionyl)pyrrolidine-2-carbonyl]amino}-2-vinylcyclopropanecarboxylic acid ethyl ester 
• 1338650-06-8 1-{[4-(4-bromobenzenesulfonyloxy)-1-(2-cyclopentyloxycarbonylamino-3-pent-4-enylsulfanylpropionyl)pyrrolidine-2-carbonyl]amino}-2-vinylcyclopropanecarboxylic acid ethyl ester 
• 1338650-07-9 1-[(4-(4-bromobenzenesulfonyloxy)-1-{2-cyclopentyloxycarbonylamino-3-[(2-nitro-benzenesulfonyl)pent-4-enyl-amino]propionyl}pyrrolidine-2-carbonyl)amino]-2-vinylcyclopropanecarboxylic acid ethyl ester 
• 1338650-08-0 1-{[1-[3-(acetyl-pent-4-enyl-amino)-2-cyclopentyloxycarbonylaminopropionyl]-4-(4-bromobenzenesulfonyloxy)pyrrolidine-2-carbonyl]amino}-2-vinylcyclopropanecarboxylic acid ethyl ester 
• 1338650-09-1 1-({4-(4-bromobenzenesulfonyloxy)-1-[2-cyclopentyloxycarbonylamino-3-(methyl-pent-4-enyl-amino)propionyl]pyrrolidine-2-carbonyl}amino)-2-vinylcyclopropanecarboxylic acid ethyl ester 
• 801282-60-0 C₂₃H₂₉BrN₂O₈S 

Relevant academic research and scientific papers

Novel, sulfonamide linked inhibitors of the hepatitis C virus NS3 protease

A sulfonamide replacement of the P2-P3 amide bond in the context of macrocyclic HCV NS3 protease inhibitors was investigated. These analogs displayed good inhibitory potency in the absence of any P3 capping group. The synthesis and preliminary SAR are des

HCV NS3 protease inhibitors

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

HCV NS3 PROTEASE INHIBITORS

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

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

HEPATITIS C INHIBITOR COMPOUNDS

Compounds of Formula (I): wherein B, R3, L0, L1, R2, Rc and R1 are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection. In particular, the present invention provides novel peptide analogs, pharmaceutical compositions containing such analogs, and uses of these analogs in the treatment of HCV infection

HEPATITIS C INHIBITOR DIPEPTIDE ANALOGS

The present invention relates to compounds of formula (I): wherein R1, R2, R4, n and m are as defined herein and R3 is selected from: (i) -C(O)OR31 wherein R31 is (C1-6)alkyl or aryl, wherein the (C1-6)alkyl is optionally substituted with one to three halogen substituents; (ii) -C(O)NR32R33, wherein R32 and R33 are each independently selected form H, (C1-6)alkyl, and Het; (iii) -SOvR34, wherein v is 1 or 2 and R34 is selected from: (C1-6)alkyl, aryl, Het, and NR32R33 wherein R32 and R33 are as defined above; and (iv) -CO(O)-R35, wherein R35 is selected from (C1-8)alkyl, (C3-7)cycloalkyl-(C1-4)alkyl, aryl, aryl-(C1-6)alkyl, Het and Het-(C1-6)alkyl, each of which are optionally substituted with one or more substituents each independently selected from halo, (C1-6)alkyl, (C3-7)cycloalkyl, aryl, Het, hydroxyl, -O-(C1-6)alkyl, -S-(C1-6)alkyl, -SO-(C1-6)alkyl, -SO2-(C1-6)alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, wherein the aryl portion of the -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one to five halo substituents. The present invention further relates to pharmaceutical compositions containing the compounds of formula (I) and methods for using these analogs in the treatment of HCV infection.