41487-76-7Relevant academic research and scientific papers
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition
Mihalic, Jeffrey T.,Fan, Pingchen,Chen, Xi,Chen, Xiaoqi,Fu, Ying,Motani, Alykhan,Liang, Lingming,Lindstrom, Michelle,Tang, Liang,Chen, Jin-Long,Jaen, Juan,Dai, Kang,Li, Leping
, p. 3781 - 3785 (2012)
An initial SAR study resulted in the identification of the novel, potent MCHR1 antagonist 2. After further profiling, compound 2 was discovered to be a potent inhibitor of the hERG potassium channel, which prevented its further development. Additional opt
Facile Synthesis of Single α-tert-Alkylated Acetaldehydes by Hydroxyalkylation of Enamides in Aqueous Solution
Murata, Yumi,Nishikata, Takashi
supporting information, p. 6354 - 6357 (2018/04/06)
In this work, we established a general protocol to synthesize single α-tert-alkylated acetaldehydes via Cu-catalyzed hydroxyalkylation of enamides in aqueous solutions. The yields of the products were very high and there was excellent functional group compatibility. Our reaction allows easy access to highly functionalized acetaldehydes that can be used to synthesize further useful compounds including spirocycles. The control experiments revealed that this reaction includes hydroxyalkylation processes via radical reactions.
SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF
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, (2011/12/02)
The present invention discloses and claims respectively a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (I) (Ia) and formula (Ib) as described herein. More specifically, the compounds of this invention
SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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, (2011/12/02)
The present invention discloses and claims a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula ( Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described her
SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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, (2011/12/02)
The present invention discloses and claims a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). (Formula (I)) Wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifical
Stereoselective synthesis of a MCHr1 antagonist
Andersen, Denise,Storz, Thomas,Liu, Pingli,Wang, Xin,Li, Leping,Fan, Pingchen,Chen, Xiaoqi,Allgeier, Alan,Burgos, Alain,Tedrow, Jason,Baum, Jean,Chen, Ying,Crockett, Rich,Huang, Liang,Syed, Rashid,Larsen, Robert D.,Martinelli, Mike
, p. 9648 - 9655 (2008/03/17)
(Chemical Equation Presented) Melanin-concentrating hormone (MCH) is implicated in the feeding behavior in mammals affording a potential target to control overeating in people. Compound 1 (AMG 076) has been identified as a potent MCHr1 antagonist for the
NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME,PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME
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Page 37-38, (2008/06/13)
There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N-R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like.The 4-(2-furoyl) aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
gem-Dichlorocyclopropanes as Masked Esters: A Novel Synthesis of β-Methoxycarbonyl Aldehydes and Ketones
Banwell, Martin G.
, p. 1453 - 1454 (2007/10/02)
The carbonyl conjugated gem-dichlorocyclopropanes (1) react with sodium methoxide in methanol affording β-methoxycarbonyl aldehydes and ketones in high yield.
