- Divergent electrolysis for the controllable coupling of thiols with 1,2-dichloroethane: A mild approach to sulfide and sulfoxide
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Organosulfurs are important commodity chemicals and indispensable synthetic intermediates in modern chemistry that were traditionally synthesized using metal catalysts, oxidants or strong bases, which caused numerous environmental pollution issues. The divergent synthesis of these scaffolds via a single catalysis under catalyst and oxidant free conditions is a fantastic idea to overcome these drawbacks. Here, we report a safe, practical and eco-friendly electrochemical methodology for the controllable dechloro-coupling of 1,2-dichloroethane (DCE) with thiols, providing value-added β-chloroethylsulfurs, which serve as versatile building blocks in the efficient late-stage conversion to bioactive molecules. The mildness and practicality of this protocol was further demonstrated by the total synthesis of anti-gout drug sulfinpyrazone in a 32% total yield over three steps.
- He, Jiaying,Ling, Changwu,Ling, Fei,Liu, Lei,Liu, Tao,Xu, Chao,Zhang, Wangqin,Zhong, Weihui
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p. 1342 - 1349
(2022/02/17)
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- Contraceptive method
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Contraceptive method comprises maintaining in the genital tract of a female mammal a pyrazolone derivative in a concentration effective to inhibit the fertilization of ova. In addition to effectively inhibiting the enzymes or other sperm components necessary for conception, the compounds used in the method of the invention are advantageous in having low toxic, caustic or irritating properties, so that the contraceptive compositions are suitable for long-term use without adverse side-effects.
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- Pharmaceutical compositions
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Supra-additive blood platelet antiaggregation activity is observed with anagrelide in combination with those non-steroidal anti-inflammatory agents which are inhibitors of platelet cyclooxygenase. The supra-additive effects of such combinations make possible new compositions and methods for both therapeutic and prophylactic treatment of thrombosis and other disorders associated with blood platelet aggregation.
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- Selective oxidation of 1,2-diphenyl-4-(2-phenylthio)ethyl)-3,5-pyrazolidinedione to the sulfinyl compound
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Herein is described a process for oxidizing 1,2-diphenyl-4-[2-(phenylthio)ethyl]-3,5-pyrazolidinedione with peroxymonosulfuric acid to obtain 1,2-diphenyl-4-[2-(phenylsulfinyl)ethyl]-3,5-pyrazolidinedione.
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