3377-20-6Relevant articles and documents
COMPOUNDS FOR SELECTIVE BINDING TO ESTROGEN RECEPTORS ALPHA/BETA RELATIVE TO GPER/GPR30
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Page/Page column 50, (2021/03/05)
The current invention is in the field of molecular biology/pharmacology and provides novel 3-oxabicyclo [3.3.1] nonene compounds and derivatives that modulate the effects of the classical estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the G protein-coupled estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and/or antagonists of one or more of the disclosed classical estrogen receptors.
Development of a Scalable Process for the Insecticidal Candidate Tyclopyrazoflor. Part 1. Evaluation of [3 + 2] Cyclization Strategies to 3-(3-Chloro-1 H-pyrazol-1-yl)pyridine
Yang, Qiang,Li, Xiaoyong,Lorsbach, Beth A.,Roth, Gary,Podhorez, David E.,Ross, Ronald,Niyaz, Noormohamed,Buysse, Ann,Knueppel, Daniel,Nissen, Jeffrey
, p. 2122 - 2132 (2019/11/02)
The evaluation of [3 + 2] cyclization strategies to prepare a key intermediate, 3-(3-chloro-1H-pyrazol-1-yl)pyridine, for the insecticidal candidate tyclopyrazoflor (1) is described. Among the validated strategies, the route involving [3 + 2] cyclization of 3-hydrazinopyridine·2HCl with methyl acrylate was selected for further optimization. This route provided ready access to 3-(3-chloro-1H-pyrazol-1-yl)pyridine in three steps via cyclization, chlorination, and oxidation. Further functionalization of 3-(3-chloro-1H-pyrazol-1-yl)pyridine via nitration, reduction, and amide formation with 3-((3,3,3-trifluoropropyl)thio)propanoic acid followed by ethylation rendered 1 in a total of seven steps.
A facile method for the synthesis of fused perhydropyrano[2,3: -b] pyrans promoted by Yb(OTf)3
Liang, Peng,Pan, Yang,Ma, Xiaofeng,Jiao, Wei,Shao, Huawu
supporting information, p. 3763 - 3766 (2018/04/17)
A stereospecific three-component domino reaction between glycals, alkylidene malonate and aldehydes catalyzed by Yb(OTf)3 is described. Multi-substituted cis-fused perhydropyrano[2,3-b]pyran derivatives were obtained with high diastereoselectiv