1233955-69-5

Upstream product

• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 
• 624-83-9 methyl isocyanate 
• 74-89-5 methylamine 
• 6452-47-7 methylcarbamoyl chloride 
• 670253-16-4 4-[(phenoxycarbonyl)amino]piperidine-1-carboxylic acid tert-butyl ester 
• 180695-80-1 tert-butyl 4-azidopiperidine-1-carboxylate 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 90633-18-4 4-bromo-1H-piperidine 

Relevant academic research and scientific papers

Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist

Analgesics with no abuse liability are highly demanded in the market. KOR agonists have been proved to be strong analgesics without MOR agonist-related side effects, such as respiratory depression, tolerance, and dependence liability; however, activation

PHENYL PROPANAMIDE DERIVATIVE, AND MANUFACTURING METHOD AND PHARMACEUTICAL APPLICATION THEREOF

The present invention provides a phenyl propanamide derivative as represented by formula (I), a manufacturing method of the derivative, application of the derivative as a κ-opioid receptor (KOR) agonist, and application of the derivative for manufacturing a pharmaceutical product for treating and/or preventing pain or a pain-related disease.

Synthesis method of 1-methyl-3-(piperidine-4-yl) urea hydrochloride

The invention relates to a synthesis method of 1-methyl-3-(piperidine-4-yl) urea hydrochloride. The synthesis method comprises the following steps: (1) reacting N-Boc-4-aminopiperidine with methylchloroformate in a solvent in the presence of organic alkali to generate N-Boc-4-[(methoxy acyl) amino] piperidine; (2) reacting N-Boc-4-[(methoxy acyl) amino] piperidine prepared in the step (1) with methylamine in the solvent in the presence of organic alkali to generate 1-methyl-3-(N-Boc-piperidine-4-yl) urea; and (3) reacting 1-methyl-3-(N-Boc-piperidine-4-yl) urea prepared in the step (2) with acetyl chloride in the solvent to obtain a final product which is 1-methyl-3-(piperidine-4-yl) urea hydrochloride. The method is easily available in raw materials, mild in reaction condition, easy to operate and high in total yield; the molar total yield of three steps of reaction, which is metered according to the raw material N-Boc-4-aminopiperidine, can reach not less than 87%; the method is applicable to industrial production.

Phenyl-propionamide derivative, and preparation method and application thereof in medicine

The invention relates to a phenyl-propionamide derivative, and a preparation method and application thereof in medicine, in particular to a phenyl-propionamide derivative shown in a general formula (I), a preparation method thereof and a medicine composition comprising the derivative, a use as a k opioid receptor (KOR receptor) agonist, and an application in preparing drugs for treating and/or preventing pains and pain-related diseases. The definition of various substituent groups of the general formula (I) is same with the definition in the description. The formula is shown in the description.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: Synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N- (benzyloxycarbonyl)amino)piperidin-1-yl)butanes

(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro (2,3-dihydrobenzthiophene-3,4′-piperidin-1′-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50 = 10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists.