131195-91-0Relevant articles and documents
Preparation method of ortho-amino trifluoroacetophenone and derivatives thereof
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Paragraph 0041; 0045-0048, (2021/11/19)
The invention relates to the field of organic synthesis, in particular to a preparation method of ortho-amino trifluoroacetophenone and derivatives thereof. The preparation of ortho-amino trifluoroacetophenone comprises three steps of amino protection, trifluoroacetylation and deprotection, the overall reaction condition is mild, the yield is high, and the method is suitable for large-scale production. In addition, on the basis of the preparation, substitution is carried out after amino diazotization, the ortho-amino trifluoroacetophenone derivative is further prepared, and the industrial application prospect is good.
Efficient Electrocatalysis for the Preparation of (Hetero)aryl Chlorides and Vinyl Chloride with 1,2-Dichloroethane
Liang, Yujie,Lin, Fengguirong,Adeli, Yeerlan,Jin, Rui,Jiao, Ning
supporting information, p. 4566 - 4570 (2019/02/14)
Although the application of 1,2-dichloroethane (DCE) as a chlorinating reagent in organic synthesis with the concomitant release of vinyl chloride as a useful byproduct is a fantastic idea, it still presents a tremendous challenge and has not yet been achieved because of the harsh dehydrochlorination conditions and the sluggish C?H chlorination process. Here we report a bifunctional electrocatalysis strategy for the catalytic dehydrochlorination of DCE at the cathode simultaneously with anodic oxidative aromatic chlorination using the released HCl as the chloride source for the efficient synthesis of value-added (hetero)aryl chlorides. The mildness and practicality of the protocol was further demonstrated by the efficient late-stage chlorination of bioactive molecules.
Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: Novel, highly potent and orally efficacious squalene synthase inhibitors
Ichikawa, Masanori,Yokomizo, Aki,Itoh, Masao,Haginoya, Noriyasu,Sugita, Kazuyuki,Usui, Hiroyuki,Terayama, Koji,Kanda, Akira
experimental part, p. 5207 - 5224 (2011/10/08)
We have recently reported the discovery of the new benzhydrol template, which has a highly potent inhibitory activity for squalene synthase, as typified by compound 1 (SSI IC50 = 0.85 nM). However, it was composed of a pair of easy rotatable at