957121-89-0

Upstream product

• 461-96-1 3,5-difluorobromobenzene 
• 459-73-4 GlyOEt*HCl 
• 220607-75-0 2-bromo-1-(3,5-difluorophenyl)ethanone 
• 1260403-67-5 C₁₄H₁₆F₂N₂O 
• 105-36-2 ethyl bromoacetate 
• 60421-23-0 cycloleucine methyl ester hydrochloride 
• 1260403-64-2 4-(3,5-difluorophenyl)-5H-[1,2,3]-oxathiazole 2,2-dioxide 
• 1260403-65-3 C₈H₇F₂NO₃S 
• 1260403-66-4 C₁₅H₂₀F₂N₂O₅S 
• 1260403-58-4 CH₄O₃S*C₁₅H₁₇F₂NO₃ 
• 1260403-60-8 CH₄O₃S*C₁₅H₁₉F₂NO₃ 
• 1260403-59-5 C₁₅H₁₉F₂NO₃ 
• 1260403-61-9 C₁₈H₁₄O₈*C₁₈H₂₂F₂N₂O₃ 
• 1260403-63-1 α-acetoxy-3,5-difluoroacetophenone 

Downstream Products

• 957121-87-8 lithium [(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]acetate 
• 1260403-61-9 C₁₈H₁₄O₈*C₁₈H₂₂F₂N₂O₃ 
• 957118-49-9 [3H]-MK 3207 
• 957187-34-7 C₁₆H₁₈F₂N₂O₃ 

Relevant academic research and scientific papers

Practical asymmetric synthesis of a chiral piperazinone derivative

A practical asymmetric route to a chiral piperazinone derivative, a fragment of MK-3207, is reported. The amine-bearing benzylic stereocenter is introduced via an asymmetric Pd-catalyzed hydrogenation of a cyclic sulfimidate in the presence of a chiral phosphine ligand. An efficient synthesis of the hydrogenation substrate is described, together with process development of the hydrogenation step and elaboration of the resulting cyclic sulfamate product to the desired piperazinone.

PROCESS FOR MAKING CGRP RECEPTOR ANTAGONIST

The invention encompasses a novel process for making 2-[(8R)-8-(3,5-Difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide, which is a CGRP receptor antagonist useful for the treatment of migraine, using an asymmetric phase-transfer catalysis route. The invention also encompasses an efficient and practical synthesis of the (R)-acid intermediate, and generates the benzylic stereocenter in an enantioselective manner.

Substituted monocyclic CGRP receptor antagonists

Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.