181641-53-2

Upstream product

• 7677-24-9 trimethylsilyl cyanide 
• 63843-83-4 1-benzyl-4-hydroxy-4-phenylpiperidine 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 172733-78-7 N-(1-benzyl-4-phenylpiperidin-4-yl)acetamide 
• 591-51-5 phenyllithium 
• 181641-49-6 1-benzyl-4-phenylpiperidin-4-ylamine 
• 109-94-4 formic acid ethyl ester 

Downstream Products

• 182621-57-4 {3-(3,4-Dichloro-phenyl)-3-[3-(4-methylamino-4-phenyl-piperidin-1-yl)-propyl]-piperidin-1-yl}-phenyl-methanone 
• 182621-56-3 4-methylamino-4-phenylpiperidine 
• 172734-92-8 (S)-(N)-(1-(3-(1-benzoyl-3(3,4-dichlorophenyl)piperidin-3-yl)propyl)-4-phenylpiperidin-4-yl)-N-methylacetamide 
• 172734-92-8 osanetant 
• 188916-70-3 N-Methyl-N-(4-phenyl-piperidin-4-yl)-acetamide; hydrochloride 
• 172734-03-1 1-Benzyl-4-(methylamino)-4-phenylpiperidine 

Relevant academic research and scientific papers

PIPERIDINE DERIVATIVES, PROCESS FOR OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula STR1 used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P-and neurokinin-dependent pathologies.

A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist

A practical and scalable total synthesis of tachykinin NK3 receptor antagonist SR 142801, (R)-N-[1-[3-[1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4 -piperidinyl]-N-methyl acetamide 1 is described. The absolute configuration of the key intermediate 7 was determined by single crystal X-ray crystallography, on the basis of which, the absolute configuration of SR 142801 should be (R)-(+), instead of the recently reported (S)-(+).

A novel modification of the Ritter reaction using trimethylsilyl cyanide

A new modification of the Ritter reaction using trimethylsilyl cyanide (Me3SiCN) is described, which converts alcohols to their corresponding formamides in high yields using a convenient procedure. The reaction conditions and mechanism are discussed. In some cases, new formamides are synthesized which cannot be prepared by the classical Ritter reaction.

A reliable and efficient synthesis of SR 142801

A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1 -yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)-(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen.