22371-32-0Relevant articles and documents
FLOW CHEMISTRY SYNTHESIS OF ISOCYANATES
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, (2021/06/22)
The disclosure provides, inter alia, safe and environmentally-friendly methods, such as flow chemistry, to synthesize isocyanates, such as methylene diphenyl diisocyanate, toluene diisocyanate, hexamethylene diisocyanate, isophorone diisocyanate, and tetramethylxylene diisocyanate.
Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor
Bhardwaj, Rajesh,Carrel, Aline Lucie,Cunha, Micael Rodrigues,Hediger, Matthias A.,Lindinger, Sonja,Parise-Filho, Roberto,Reymond, Jean-Louis,Romanin, Christoph
supporting information, p. 1032 - 1040 (2020/10/06)
Transient receptor potential vanilloid 6 (TRPV6) is a calcium channel implicated in multifactorial diseases and overexpressed in numerous cancers. We recently reported the phenyl-cyclohexyl-piperazine cis-22a as the first submicromolar TRPV6 inhibitor. This inhibitor showed a seven-fold selectivity against the closely related calcium channel TRPV5 and no activity on store-operated calcium channels (SOC), but very significant off-target effects and low microsomal stability. Here, we surveyed analogues incorporating structural features of the natural product capsaicin and identified 3OG, a new oxygenated analog with similar potency against TRPV6 (IC50 = 0.082 ± 0.004 μM) and ion channel selectivity, but with high microsomal stability and very low off-target effects. This natural product-inspired inhibitor does not exhibit any non-specific toxicity effects on various cell lines and is proposed as a new tool compound to test pharmacological inhibition of TRPV6 mediated calcium flux in disease models.
Parameters of synthesis of hydrazides and 1,2-diacylhydrazines by thermal decomposition of hydrazine salts of aliphatic carboxylic acids
Drozdetskii,Radushev,Turbin,Gusev,Drozdova,Shekhonina,Chekanova
, p. 302 - 306 (2007/10/03)
The reaction parameters were refined for synthesis of hydrazides and 1,2-diacylhydrazines by thermal decomposition of salts of aliphatic carboxylic acids of the general formulas RCOOH · N2H4 · H2O and 2RCOOH-N2H4-H2O (R = C2H5-C8H17). Derivatograms for series of compounds were obtained. The effect of hydrazine hydrate excess, temperature, reaction duration, and crystallization conditions on the yield and quality of hydrazides of C7-C9 carboxylic acids was studied.