1456-72-0Relevant articles and documents
Preparation method of 1, 3, 4-thiadiazole compound and compound prepared by preparation method
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Paragraph 0019-0020; 0039-0040, (2020/12/10)
The invention belongs to the field of medicinal chemistry. Specifically, the invention discloses a preparation method of a 1, 3, 4-thiadiazole compound and the compound prepared by using the preparation method. According to the method, the 1, 3, 4-thiadia
A KHSO4 promoted tandem synthesis of 1,3,4-thiadiazoles from thiohydrazides and DMF derivatives
Gan, Zongjie,Tian, Binghua,Yuan, Jianyong,Ran, Dongzhi,Zhang, Lin,Dong, Gang,Pan, Tao,Zeng, Yixin,Yu, Yu
supporting information, (2020/07/15)
An efficient, simple and environmentally benign method for the construction of 1,3,4-thiadiazole skeletons via the tandem coupling and cyclization of thiohydrazides with DMF derivatives in the presence of KHSO4 has been reported. This method re
Ring opening of pymisyl-protected aziridines with organocuprates
Bornholdt, Jan,Felding, Jakob,Clausen, Rasmus P.,Kristensen, Jesper L.
supporting information; experimental part, p. 12474 - 12480 (2010/12/25)
The pyrimidine-2-sulfonyl (pymisyl) group is introduced as a new protecting group that can be used to activate aziridines towards ring opening. It is readily introduced and removed under mild conditions. Regioselective ring opening of pymisyl-protected 2-methyl-aziridine with organocuprates gives the corresponding sulfonamides in high yields, and the pymisyl group can subsequently be removed upon treatment with a thiolate. The versatility of this new nitrogen protecting group is illustrated with a new synthesis of Selegiline, a monoamine oxidase-B inhibitor marketed for the treatment of Parkinson's disease. Easy on'easy off: The pymisyl group is introduced as a new protecting group for the activation of aziridines towards ring opening with organocuprates (see scheme). It is readily removed under very mild conditions with thiolates. The versatility of the approach is illustrated in a new synthesis of Selegiline, a drug marketed for the treatment of Parkinson's disease.