380629-65-2

Upstream product

• 100-39-0 benzyl bromide 
• 76944-95-1 tert-butyl N-[(3S)-2-oxoazepan-3-yl]carbamate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 21568-87-6 2-aminocaprolactam 
• 1389338-67-3 C₂₀H₂₈N₂O₃ 
• 90600-20-7 (2S)-2-[(tert-butoxycarbonyl)amino]pent-4-enoic acid 
• 1055423-27-2 (3S)-3-[[(1,1-dimethylethoxy)carbonyl]amino]hexahydro-2-oxo-1H-azepine-1-carboxylic acid phenylmethyl ester 
• 2389-45-9 Boc-Lys(Z)-OH 

Downstream Products

• 918437-67-9 7-benzyl-1-tert-butoxycarbonyl-1,7-diaza-spiro[4,6]undec-6-one 
• 918437-66-8 tert-butyl (S)-1-benzyl-2-oxazepan-3-yl-3-bromopropylcarbamate 
• 918437-79-3 (1-benzyl-2-oxo-azepan-3-yl)-(3-hydroxy-propyl)-carbamic acid tert-butyl ester 
• 1361322-55-5 (S)-N-((S)-1-cyclohexyl-2-oxo-2-((S)-1-phenethylazepan-3-ylamino)ethyl)-2-(methylamino)propanamide 
• 1361323-06-9 tert-butyl (S)-1-((S)-1-cyclohexyl-2-oxo-2-((S)-1-phenethylazepan-3-ylamino)ethylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 1361322-54-4 (S)-N-((S)-2-((S)-1-benzylazepan-3-ylamino)-1-cyclohexyl-2-oxoethyl)-2-(methylamino)propanamide 
• 1361323-05-8 tert-butyl (S)-1-((S)-2-((S)-1-benzylazepan-3-ylamino)-1-cyclohexyl-2-oxoethylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 1361378-83-7 (S)-2-amino-N-((S)-1-benzylazepan-3-yl)-2-cyclohexylacetamide dihydrochloride 
• 1361323-03-6 tert-butyl (S)-2-((S)-1-benzylazepan-3-ylamino)-1-cyclohexyl-2-oxoethylcarbamate 
• 625471-23-0 (S)-1-benzylazepan-3-amine 
• 202819-52-1 (RS)-3-amino-2-oxo-1-benzyl-azepine 
• 635754-92-6 (S)-4-{[(1-trityl-1H-imidazol-4-ylmethyl)-(1-benzyl-2-oxo-azepan-3-yl)-amino]-methyl}-benzonitrile 
• 635754-91-5 (S)-1-benzyl-3-[(1-trityl-imidazol-4-ylmethyl)amino]-azepan-2-one 

Relevant academic research and scientific papers

Ring-closing metathesis based total synthesis of ciliatamides A and B and their structural confirmation

Protecting group dependant ring-closing metathesis based approach to the total synthesis of the revised structures of ciliatamides A and B has been described. The current synthetic strategy utilizes the amino acid as starting material to introduce both the stereogenic centers. However, usage of non-racemizing reagents (EDC·HCl, HATU/NMM); for amide coupling and Grubbs' second generation catalyst for caprolactam ring synthesis makes the present approach more convenient to get the correct conclusion on absolute stereochemistry. Thus, on the basis of similar optical rotation values with the Lindsley's reported data, this synthesis further supported for the actual stereochemistry of both ciliatamides A and B is (R,R).

SUBSTITUTED ADIPIC ACID AMIDES AND USES THEREOF

The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1 C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.

Discovery of aminopiperidine-based Smac mimetics as IAP antagonists

A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously described Smac mimetics contain the proline ring (or a similar cyclic motif) found in Smac, a key feature of the compounds described herein is that this ring has been removed. Despite this, compounds in this series potently bind to cIAP1 and elicit the expected phenotype of cIAP1 inhibition in cancer cells. Marked selectivity for cIAP1 over XIAP is observed for these compounds, which is attributed to a slight difference in the binding groove between the two proteins and the resulting steric interactions with the inhibitors. XIAP binding can be improved by constraining the inhibitor so that these unfavorable steric interactions are minimized.

Stereochemical diversity in asymmetric cyclization via memory of chirality

An enantiodivergent asymmetric cyclization of N-Boc-N-ω-bromoalkyl-α-amino acid derivatives has been developed. With potassium amide bases in DMF, cyclization proceeds with retention of configuration, while inversion of configuration was observed with lit

SUBSTITUTED QUINOLINE CCR5 RECEPTOR ANTAGONISTS

The present invention relates to CCR5 receptor antagonists of formulae (1a) or (1b), enantiomers, diastereomers, salts and solvates thereof wherein R1, R2, R3, R4, R5, and R7 are as defined herein. The invention further includes a method of CCR5-mediated

Parallel liquid synthesis of N,N′-disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors

A rapid structure-activity study was performed by parallel liquid synthesis on N,N′-disubstitution of 3-amino azepin-2-one to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities. The activities of the selected compounds were validated in vivo, and compounds 41a and 44a presented significant antitumour activity.

Lactam inhibitors of factor Xa and method

Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, 1011 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.