1195758-84-9

Upstream product

• 342578-12-5 C₁₁H₂₁NO₄S 
• 1776-53-0 4-aminocyclohexanecarboxylic acid 

Downstream Products

• 1192424-59-1 C₁₅H₂₇NO₅S 
• 1192424-61-5 C₁₃H₂₃N₃O₃S 
• 1192424-63-7 C₁₄H₂₂F₃N₃O₅S₂ 
• 1192424-65-9 C₁₉H₂₆FN₃O₂S 
• 1192424-67-1 C₁₉H₂₅FIN₃O₂S 
• 1192424-69-3 C₂₀H₂₅FN₄O₂S 
• 342577-38-2 Velneperit 

Relevant academic research and scientific papers

Development of an optimized synthetic and purification process of S-2367 (Velneperit), a novel neuropeptide y (NPY) Y5 receptor antagonist

We developed a simple synthetic route to S-2367 (Velneperit) (1) using trans-1-ethoxycarbonyl-4-aminocyclohexane hydrochloride salt (12) as a starting material. The key step was Na2WO4/H2O2 oxidation, and we found that it was accelerated in weakly basic conditions. The finding was useful to control one of the critical impurities: 14 in 10. The new process was more efficient than the early process from the viewpoint of the number of reactions, yield, throughput, and EHS (environment, health, and safety) but a quality deviation occurred in the pilot manufacturing: 10 content in 1 was over the upper limit. The cause was presumed to be hydrolysis of 1 during the recrystallization step. After finding it, we developed two reliable purification processes. The first was slurry washing including clever polymorphic control using only acetone and water. The second was salt formation of 10 and rational building of the recrystallization procedure based on solubility to improve removal rate.

COMPOUND HAVING NPY Y5 RECEPTOR ANTAGONIST ACTIVITY

This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.