656-65-5Relevant academic research and scientific papers
Synthesis method of tedizolid phosphate intermediate 3-fluoro-4-bromoaniline
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, (2020/12/09)
The invention provides a synthesis method of a tedizolid phosphate intermediate 3-fluoro-4-bromoaniline. The synthesis method comprises the following steps: (1) performing reacting of a compound 1 with ammonia gas to obtain a compound 2; (2) performing reacting of the compound 2 with hydrobromic acid to obtain a compound 3; and (3) reducing a cyano group in the compound 3 into an amino group to obtain a compound 4. The raw material adopted by the method is cheap and easy to obtain, and the method is mild in reaction condition, simple in equipment requirement, high in safety index and suitablefor large-scale commercial production. The yield of the tedizolid phosphate intermediate 3-fluoro-4-bromoaniline prepared by the process provided by the invention is up to 56.61% or above, the purityis up to 99.70% or above, and the content of isomer impurities in the product is as low as 0.17% or below. The invention provides the cheap and easily available high-quality intermediate for commercial production of tedizolid phosphate bulk drugs, and a wide application prospect is achieved.
Cu-mediated selective bromination of aniline derivatives and preliminary mechanism study
Zhao, Hong-Yi,Yang, Xue-Yan,Lei, Hao,Xin, Minhang,Zhang, San-Qi
supporting information, p. 1406 - 1415 (2019/05/01)
A simple and efficient bromination of aniline, aniline derivatives, and analogs have been developed. Forty three examples were given and the highest yield reached was 98%. Different substrates including substituted aniline, pyridin-amine, N-substituted aniline, N,N-disubstituted aniline, N-phenyl-amide, N-phenyl-sulfonamide, and nitrogen-containing heterocycles were all reactive and selectively generated desired bromo-products. The method can be applied to synthesize drug intermediate and quinoxaline derivatives.
SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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, (2015/01/07)
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Regioselective chlorination and bromination of unprotected anilines under mild conditions using copper halides in ionic liquids
Wang, Han,Wen, Kun,Nurahmat, Nurbiya,Shao, Yan,Zhang, He,Wei, Chao,Li, Ya,Shen, Yongjia,Sun, Zhihua
supporting information; experimental part, p. 744 - 748 (2012/06/30)
By using ionic liquids as solvents, the chlorination or bromination of unprotected anilines at the para-position can be achieved in high yields with copper halides under mild conditions, without the need for potentially hazardous operations such as supplementing oxygen or gaseous HCl.
Electrophilic bromination of meta-substituted anilines with N-bromosuccinimide: Regioselectivity and solvent effect
Bartoli, Sandra,Cipollone, Amalia,Squarcia, Antonella,Madami, Andrea,Fattori, Daniela
experimental part, p. 1305 - 1308 (2009/12/24)
N-Bromosuccinimide-mediated electrophilic aromatic bromination of a series of anilines substituted with an electron-with-drawing group in the meta position was investigated. The regioselectivity of the reaction is markedly dependent on the polarity of the solvent and the bromination reaction can be tuned by appropriate selection of the reaction medium. Georg Thieme Verlag Stuttgart.
Anisotropic organic compounds
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, (2008/06/13)
STR1 The invention describes liquid crystalline compounds or formula (I), where A, D and G are independently selected from phenyl, thiophene, hydrogenated phenyl, chlorinated phenyl and fluorinated phenyl, B and E are independently selected from a single bond C= C. C C.C00, azoxy and diazo, k and m are independently selected from 1 and 0, such that m+n is 1 or 2, and R1 and R2 are independently selected from R, R0, alkynyl, thioalkyl, hydrogen, CN, NCS and SCN; provided that at least one of R1 and R2 is selected from CN, NCS and SCN and that at least one of A, D and G is phenyl; and excluding where at least one of R1 and R2 is independently selected as CN and one of A, D or G is not thiophene, and where m is 0, A, and D are phenyl, B is a single bond and only one of R1 or R2 is NCS. Also described are compounds suitable for inclusion in a device utilizing pretransitional characteristics of liquid crystalline materials in the isotropic phase, of general formula (II) where J and Y are independently selected from phenyl, thiophene, hydrogenated phenyl, chlorinated phenyl and fluorinated phenyl, X is selected from C= C. C C.COO azoxy and diazo, k is 1 or 0 and R3 and R4 are independently selected from R, RO, alkynyl, thioalkyl, hydrogen, CN, NCS and SCN; provided that at least one of R3 and R4 is selected from CN, NCS and SCN and that at least one of J and Y is phenyl.
The Synthesis of Several Lateral Difluoro-substituted 4,4''-Dialkyl- and 4,4''-Alkoxyalkyl-Terphenyls and a Rationalisation of the Effect of Such Substitution on Mesophase Type and Transition Temperatures
Gray, G. W.,Hird, M.,Toyne, K. J.
, p. 43 - 64 (2007/10/02)
In recent years we have prepared a large number of mono-fluoro- and ortho-difluoro-substituted 4,4''-dialkyl- and 4,4''-alkoxyalkyl-terphenyls.The synthesis and transition temperatures of a variety of related difluoro compounds is presented here so that it is now possible to identify (i) broadening of the molecule, (ii) twisting about an inter-annular bond, and (iii) the presence of an "inner" (2-, 2'-, 3'- or 2''-substituent) or an "outer" (3- or 3''-substituent) fluorine, as being the major factors which influence the type and the thermal stability of the mesophases obtained.
