135206-87-0Relevant articles and documents
Triazole alcohol derivative as well as preparation method and application thereof
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Paragraph 0101; 0110-0112, (2020/03/11)
The invention relates to a triazole alcohol derivative as well as a preparation method and application thereof. The chemical structure of the triazole alcohol derivative is shown as a formula I, R1 represents a benzene ring or a substituted benzene ring, and substituent groups of the substituted benzene ring can be located at all positions of the benzene ring, can be mono-substituted or multi-substituted, and can be selected from a) halogen which is F and Cl; b) an electron withdrawing group which is cyano or trifluoromethyl; c ) a lower alkyl of 1-4 carbon atoms or a halogen substituted loweralkyl; and d) lower alkoxy of 1-4 carbon atoms or halogen substituted lower alkoxy. The compound of the invention has strong antifungal activity, has the advantages of low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal drugs.
Triazole alcohol derivative, and preparation method and application thereof
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Paragraph 0109-0111, (2020/05/01)
The invention relates to a triazole alcohol derivative, and a preparation method and an application thereof. The chemical structure of the triazole alcohol derivative is represented by formula I, A inthe formula I represents a benzene ring or a substituted benzene ring, and the substituent group of the substituted benzene ring can be located at each position of the benzene ring, is monosubstituted or polysubstituted, and is selected from: a) halogen which is F, Cl, Br or I; b) an electron-withdrawing group, wherein the electron withdrawing group is a cyano group, a nitro group or a trifluoromethyl group; c) a C1-4 low alkyl group or a halogen-substituted low alkyl group; and d) a C1-4 low alkoxy group or a halogen-substituted low alkoxy group. The compound has the advantages of high antifungal activity, low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal medicines.
A PROCESS FOR THE PREPARATION OF ISAVUCONAZOLE AND ITS INTERMEDIATES
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Page/Page column 15; 16, (2015/11/17)
The present invention relates to a process for the preparation of Isavuconazole or its pharmaceutical acceptable salt thereof. In particular aspects of the present invention relates to a process for the preparation of intermediate of azole intermediate. In a further aspect, the present invention relates to a process for the preparation of triazole intermediate. In a further aspect, the present invention relates to a process for the preparation of oxirane intermediate.
Enantioselective organocatalytic rearrangement of α-acyloxy- β-keto sulfides to α-acyloxy thioesters
Capitta, Francesca,Frongia, Angelo,Piras, Pier Paolo,Pitzanti, Patrizia,Secci, Francesco
supporting information; experimental part, p. 2955 - 2960 (2011/02/22)
The first highly enantioselective organocatalytic rearrangement of α-acyloxy-β-keto sulfides to α-acyloxy thioesters has been developed which provides a number of important synthetic building blocks in high yield and with excellent enantioselectivities (e
The process development of ravuconazole: An efficient multikilogram scale preparation of an antifungal agent
Pesti, Jaan,Chen, Chien-Kuang,Spangler, Lori,DelMonte, Albert J.,Benoit, Serge,Berglund, Derek,Xbien, Derek,Brodfuehrer, Paul,Chan, Yeung,Corbett, Elisabeth,Costello, Carrie,DeMena, Paul,Discordia, Robert P.,Doubleday, Wendel,Gao, Zhinong,Gingras, Stephane,Grosso, John,Haas, Oscar,Kacsur, David,Lai, Chiajen,Leung, Simon,Miller, Melanie,Muslehiddinoglu, Jale,Nguyen, Nina,Qiu, Jun,Olzog, Martina,Reiff, Emily,Thoraval, Dominique,Totleben, Michael,Vanyo, Dale,Vemishetti, Purushotham,Wasylak, John,Wei, Chenkou
experimental part, p. 716 - 728 (2010/04/22)
The development of a safe, robust process for the preparation of ravuconazole (1), an antifungal agent, is described. The discovery and development of procedures enabling the efficient synthesis of multikilogram quantities of 1 and the process demonstration through plant scale preparations are presented. A controlled means to prepare a Grignard reagent and utilization of Fourier Transform Infrared spectroscopy (FTIR) monitoring to safely conduct the reaction is featured.
Discovery of novel indazole-linked triazoles as antifungal agents
Park, Joon Seok,Yu, Kyung A,Kang, Tae Hee,Kim, Sunghoon,Suh, Young-Ger
, p. 3486 - 3490 (2008/02/11)
The in vitro and in vivo activities of a series of (2R, 3R)-2-(2,4-difluorophenyl)-3-(substituted indazol-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol as potential antifungal agents are described. In particular, the analog 12j having 5-bromo substitution on the indazole ring exhibited significant antifungal activity against a variety of fungal cultures (Candida spp. and Aspergillus spp.). In addition, oral administration of 12j showed its excellent efficacy against Candida albicans in a murine infection model and the significantly improved survival rates of the infected mice.
NOVEL HETEROARYL DERIVATIVE
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, (2008/06/13)
A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
NOVEL HETEROARYL DERIVATIVE
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Page/Page column 86-87, (2008/06/13)
A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. (1) wherein: the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl, etc.
ANTIFUNGAL AZOLE DERIVATIVES HAVING A FLUOROVINYL MOIETY AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 11, (2010/02/10)
An azole derivative of formula (I) having a fluorovinyl moiety or a pharmaceutically acceptable salt thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.
PYRROLE DERIVATIVE
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Page 85, (2010/02/06)
A novel pyrrole derivative represented by the following formula (1) and a salt thereof: wherein R1 means substituted alkenyl, etc.; R2 means substituted benzoyl, etc.; and R3 to R5 each means hydrogen, alkyl, halogeno, etc. The derivative and salt have antidiabetic activity.