302341-61-3

Basic information

• Product Name: tert-butyl N-[(6-cyanopyridin-3- yl)Methyl]carbaMate
• Synonyms: tert-butyl N-[(6-cyanopyridin-3- yl)Methyl]carbaMate;3-(BOC-AMINOMETHYL)-6-CYANOPYRIDINE;TERT-BUTYL ((6-CYANOPYRIDIN-3-YL)METHYL)CARBAMATE
• CAS NO: 302341-61-3
• Molecular Formula: C₁₂H₁₅N₃O₂
• Molecular Weight: 233.2664
• Mol File: 302341-61-3.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: tert-butyl N-[(6-cyanopyridin-3- yl)Methyl]carbaMate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl N-[(6-cyanopyridin-3- yl)Methyl]carbaMate(302341-61-3)
• EPA Substance Registry System: tert-butyl N-[(6-cyanopyridin-3- yl)Methyl]carbaMate(302341-61-3)

Safety Data

• Hazardous Substances Data: 302341-61-3(Hazardous Substances Data)

Upstream product

• 181130-13-2 5-(azidomethyl)pyridine-2-carbonitrile 
• 24424-99-5 di-tert-butyl dicarbonate 
• 89809-65-4 methyl 6-cyanopyridine-3-carboxylate 
• 26218-78-0 methyl 6-bromonicotinate 
• 181130-14-3 5-(aminomethyl)pyridine-2-carbonitrile 
• 58553-48-3 5-(hydroxymethyl)pyridine-2-carbonitrile 
• 557-21-1 dicyanozinc 
• 285119-72-4 (6-chloropyridin-3-ylmethyl)carbamic acid tert-butyl ester 
• 41051-03-0 ethyl 5-cyano-2-pyridinecarboxylate 
• 17874-78-1 6-ethoxycarbonylpyridine-3-carboxylic acid 
• 100-26-5 Pyridine-2,5-dicarboxylic acid 
• 65346-04-5 5-cyano-2-pyridinecarboxamide 
• 100-54-9 pyridine-3-carbonitrile 
• 67515-95-1 5-chlorocarbonyl-pyridine-2-carboxylic acid ethyl ester 

Downstream Products

• 609345-79-1 5-(aminomethyl)pyridine-2-carboximidamide 
• 928649-09-6 tert-butyl N-[(6-hydroxymethyl-3-pyridyl)methyl]carbamate 
• 788801-45-6 [tert-butoxycarbonyl-(1-cyclohexylmethyl-2-{2-[(6-methylsulfanylcarbonimidoyl-pyridin-3-ylmethyl)-carbamoyl]-2,5-dihydro-pyrrol-1-yl}-2-oxo-ethyl)-amino]-acetic acid tert-butyl ester 
• 182291-44-7 [tert-butoxycarbonyl-(1-cyclohexylmethyl-2-oxo-2-{2-[(6-thiocarbamoyl-pyridin-3-ylmethyl)-carbamoyl]-2,5-dihydro-pyrrol-1-yl}-ethyl)-amino]-acetic acid tert-butyl ester 
• 182291-43-6 tert-butyl {(tert-butoxycarbonyl)[(1R)-2-[(2S)-2-({[(6-cyano-3-pyridinyl)methyl]amino}carbonyl)-2,5-dihydro-1H-pyrrol-1-yl]-1-(cyclohexylmethyl)-2-oxoethyl]amino}acetate 

Relevant articles and documents

Improving the Selectivity of PACE4 Inhibitors through Modifications of the P1 Residue

Paired basic amino acid cleaving enzyme 4 (PACE4), a serine endoprotease of the proprotein convertases family, has been recognized as a promising target for prostate cancer. We previously reported a selective and potent peptide-based inhibitor for PACE4, named the multi-Leu peptide (Ac-LLLLRVKR-NH2 sequence), which was then modified into a more potent and stable compound named C23 with the following structure: Ac-dLeu-LLLRVK-Amba (Amba: 4-amidinobenzylamide). Despite improvements in both in vitro and in vivo profiles of C23, its selectivity for PACE4 over furin was significantly reduced. We examined other Arg-mimetics instead of Amba to regain the lost selectivity. Our results indicated that the replacement of Amba with 5-(aminomethyl)picolinimidamide increased affinity for PACE4 and restored selectivity. Our results also provide a better insight on how structural differences between S1 pockets of PACE4 and furin could be employed in the rational design of selective inhibitors.

6-ARYLALKYLAMINO- 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINES AS 5-HT2C RECEPTOR AGONISTS

The present invention provides 6-substituted 2,3,4,5-tetrahydro-lH- benzo[d]azepines of Formula (I) as selective 5-HT2c receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety, where, R6 is -NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl and other substituents are as defined in the specification.

Technical scale synthesis of a new and highly potent thrombin inhibitor

In this account, we describe the development of an efficient and convergent process for the peptidomimetic thrombin inhibitor 1 on production plant scale. Starting from nicotinonitrile (13), (2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxy-2- pyrrolidinecarboxylic acid (5) and (2R)-2-amino-3-cyclohexylpropanoic acid (29) compound 1 was obtained in 16 chemical steps. New methods had been developed for the preparation of the key intermediate dehydroproline 22 and the transformation of nitriles into amidines. The thrombin inhibitor 1 was isolated by special techniques (nanofiltration and spray drying). Almost all salts of 1 are amorphous, however, a crystalline complex was obtained with 1,2-benzisothiazol-3(2H)-one 1,1-dioxide (Saccharin).

Mandelic acid derivatives and their use as throbin inhibitors

There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

PHARMACEUTICAL COMBINATION

There is provided a combination product comprising: (1) a compound of claim 1 in WO 02/44145 or a compound of claim 20 in WO 02/44145 (or derivative thereof)or a pharmaceutically-acceptable derivative thereof; and (1) a compound as defined in claim 1 of WO 01/28992 or (2) a compound of Claim 34 of WO 01/28992 or (3) Compound A or B or C or D (or pharmaceutically-acceptable salts thereof) for use in treating arrhythmia or a coagulation controlled complication thereof.