335428-62-1Relevant articles and documents
Synthesis method of garafloxacin intermediate
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Paragraph 0025; 0040; 0047-0049; 0050; 0057-0059, (2021/09/26)
The invention discloses a synthesis method of a garafloxacin intermediate (1R)-5-bromo-2, 3-dihydro-1-methyl-1H-isoindole; the synthesis method comprises the following steps of: taking a garafloxacin intermediate as a raw material; the method comprises the following steps: step 1, by taking R(+)-alpha-phenylethylamine as a raw material and lewis acid as a catalyst, carrying out bromine bromination reaction to obtain a compound 2; 2, placing the compound 2 in a solvent, adding hydrochloric acid, paraformaldehyde and a catalyst, and carrying out chloromethylation reaction to obtain a compound 3; 3, dissolving the compound 3 in a solvent, adding alkali, and heating the mixture for reaction to obtain a compound 1. The method is simple in reaction, short in route, less in three wastes, environment-friendly, high in yield of each step, less in waste of raw materials and reagents, and especially suitable for industrial production.
Traceless Directing Group Assisted Cobalt-Catalyzed C?H Carbonylation of Benzylamines
Ling, Fei,Ai, Chongren,Lv, Yaping,Zhong, Weihui
supporting information, p. 3707 - 3712 (2017/10/07)
The first example of cobalt-catalyzed C(sp2)?H carbonylation of benzylamines using a traceless directing group is reported, which was successfully applied to the synthesis of N?unprotected iso-indolinones through direct C?H/N?H bonds activation. This protocol tolerates a variety of functional groups and provides a facile and efficient method for the formal synthesis of (+)-garenoxacin. (Figure presented.).
NOVEL COMPOUND WITH ANTIBACTERIAL ACTIVITY
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, (2016/04/26)
A compound represented by the general formula (I) or a salt thereof having a potent antibacterial activity against bacteria that have acquired resistance to quinolones, and a medicament for prophylactic and/or therapeutic treatment of an infectious disease containing the compound or a salt thereof as an active ingredient, as well as a medicament for prophylactic and/or therapeutic treatment of an infectious disease containing a combination of the compound or a salt thereof, and a quinolone.