1227685-41-7

Upstream product

• 67-56-1 methanol 
• 372-19-0 meta-fluoroaniline 
• 1227685-18-8 benzyl (2S,4S)-4-hydroxy-2-methyl-4-(trichloromethyl)-piperidine-1-carboxylate 
• 921599-74-8 benzyl (2S)-2-methyl-4-oxopiperidine-1-carboxylate 
• 849928-34-3 benzyl 2-methyl-4-oxopiperidine-1-carboxylate 
• 620-08-6 4-methoxypyridine 
• 501-53-1 benzyl chloroformate 
• 190906-91-3 3,4-dihydro-2-methyl-4-oxo-1(2H)-pyridinecarboxylic acid phenylmethyl ester 

Downstream Products

• 1227685-42-8 benzyl (2S,4R)-4-[(3-fluorophenyl)amino]-4-(hydroxymethyl)-2-methylpiperidine-1-carboxylate 
• 1416161-82-4 1-benzyl 4-methyl (2S,4R)-4-[(3-ethoxy-3-oxopropanoyl)(3-fluorophenyl)amino]-2-methylpiperidine-1,4-dicarboxylate 
• 1227685-11-1 benzyl (2S,4R)-4-cyano-4-[(3-ethoxy-3-oxopropanoyl)(3-fluorophenyl)amino]-2-methylpiperidine-1-carboxylate 
• 1227685-13-3 benzyl (5R,7S)-1-(3-fluorophenyl)-4-hydroxy-7-methyl-2-oxo-1,8-diazaspiro[4.5]decane-8-carboxylate 
• 1227685-14-4 (5R,7S)-benzyl 1-(3-fluorophenyl)-7-methyl-2-oxo-1,8-diazaspiro[4.5]dec-3-ene-8-carboxylate 
• 1416161-83-5 8-benzyl 3-ethyl (5R,7S)-1-(3-fluorophenyl)-7-methyl-2,4-dioxo-1,8-diazaspiro[4.5]decane-3,8-dicarboxylate 
• 1416161-72-2 (5R,7S)-1-(3-fluorophenyl)-8-[4-hydroxy-3-(5-methyl-1H-pyrazol-1-yl)benzyl]-7-methyl-1,8-diazaspiro[4.5]dec-3-en-2-one 

Relevant academic research and scientific papers

Cyclic 1-(Arylamino)carboxylates via Mild Diastereospecific Jocic-Type Reaction with 2,2,2-Trichloromethyl Carbinols and Anilines

A mild, practical Jocic-type rearrangement for the synthesis of cyclic 1-(arylamino) carboxylates from readily available 2,2,2-trichloromethyl carbinols and anilines is described. The method demonstrates good scope, with a large variety of anilines providing direct access to several novel cyclic 1-(arylamino) carboxylates. The reaction is robust and has been shown to provide comparable results on kilogram scale. The reaction is diastereospecific, leading to the formation of a single diastereomer when utilizing stereodefined 2,2,2-trichloromethyl carbinol cores.

Process development and scale-up of a β-secretase inhibitor via a stereospecific jocic reaction

A scalable process for the synthesis of a spiropiperidine β-secretase inhibitor is described. Key stereochemical transformations utilized are a diastereoselective trichloromethyl addition followed by an unprecedented stereospecific Jocic reaction with an aniline nucleophile. Simplified processing was developed for a Dieckmann cyclization/decarboxylation sequence to give a process suitable for the production of kilogram quantities of API.

LACTAMS AS BETA SECRETASE INHIBITORS

Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermedia

LACTAMS AS BETA SECRETASE INHIBITORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis,