135270-06-3

Upstream product

• 132507-89-2 threo-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2,3-butanediol 
• 124-63-0 methanesulfonyl chloride 
• 132507-89-2 (2R,3S)-2-(2,4-Difluoro-phenyl)-1-[1,2,4]triazol-1-yl-butane-2,3-diol 
• 126918-20-5 (2R^*,3R^*)-2-(2,4-Difluorophenyl)-1,2,3-butanetriol 
• 132563-81-6 1-(2,4-difluorophenyl)-2-(tetrahydropyranyloxy)propan-1-one 
• 126918-19-2 (2S,3S)-2-(2,4-Difluoro-phenyl)-3-(tetrahydro-pyran-2-yloxy)-butane-1,2-diol 
• 126918-18-1 (2S^*,3R^*)-2-(2,4-Difluorophenyl)-1-(dimethylisopropoxysilyl)-3-(tetrahydropyran-2-yloxy)-2-butanol 
• 126918-21-6 (2R^*,3R^*)-2-(2,4-Difluorophenyl)-1,3-bis(methanesulfonyloxy)-2-butanol 
• 132507-77-8 Trifluoro-acetic acid (1R,2S)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl ester 
• 124627-86-7 (2R^*,3S^*)-2-(2,4-Difluorophenyl)-3-methyl-2-<(1H-1,2,4-triazol-1-yl)methyl>oxirane 
• 126945-34-4 Methanesulfonic acid (1S,2S)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl ester 
• 132507-89-2 (2R,3R)-2-(2,4-Difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-2,3-butanediol 
• 127001-03-0 (2R)-2',4'-Difluoro-2-(3,4,5,6-tetrahydro-2H-pyran-2-yloxy)propiophenone 
• 212890-35-2 2-[(1R)-1-(3,4,5,6-Tetrahydro-2H-pyran-2-yl)oxyethyl]-2-(2,4-difluorophenyl)oxirane 

Downstream Products

• 124627-86-7 (2R^*,3S^*)-2-(2,4-Difluorophenyl)-3-methyl-2-<(1H-1,2,4-triazol-1-yl)methyl>oxirane 
• 132507-77-8 Trifluoro-acetic acid (1R,2S)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl ester 
• 126917-19-9 (E)-1-[(4S,5S)-5-(2,4-Difluoro-phenyl)-4-methyl-5-[1,2,4]triazol-1-ylmethyl-oxazolidin-3-yl]-3-(4-trifluoromethyl-phenyl)-propenone 
• 124627-86-7 1-[(2S,3S)-2-(2,4-Difluoro-phenyl)-3-methyl-oxiranylmethyl]-1H-[1,2,4]triazole 
• 126916-57-2 (2R*,3R*)-3-Amino-2-(2,4-difluoropropyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol 
• 126916-57-2 (2R,3S)-3-Amino-2-(2,4-difluoro-phenyl)-1-[1,2,4]triazol-1-yl-butan-2-ol 
• 132507-89-2 (2R,3S)-2-(2,4-Difluoro-phenyl)-1-[1,2,4]triazol-1-yl-butane-2,3-diol 
• 126916-45-8 (4R*,5R*)-5-(2,4-Difluorophenyl)-4-methyl-5-<(1H-1,2,4-triazol-1-yl)methyl>oxazolidine 
• 126916-45-8 1-[(4R,5S)-5-(2,4-Difluoro-phenyl)-4-methyl-oxazolidin-5-ylmethyl]-1H-[1,2,4]triazole 
• 126945-34-4 Methanesulfonic acid (1R,2S)-2-(2,4-difluoro-phenyl)-2-hydroxy-1-methyl-3-[1,2,4]triazol-1-yl-propyl ester 
• 132507-72-3 (4R^*,5R^*)-5-(2,4-Difluorophenyl)-4-methyl-3-(5-methyl-4-hexenoyl)-5-<(1H-1,2,4-triazol-1-yl)methyl>oxazolidine 
• 126916-84-5 (4-Chloro-phenyl)-[(4R,5R)-5-(2,4-difluoro-phenyl)-4-methyl-5-[1,2,4]triazol-1-ylmethyl-oxazolidin-3-yl]-methanone 
• 126917-17-7 (E)-3-(4-Chloro-phenyl)-1-[(4S,5S)-5-(2,4-difluoro-phenyl)-4-methyl-5-[1,2,4]triazol-1-ylmethyl-oxazolidin-3-yl]-propenone 
• 126916-89-0 [(4R,5R)-5-(2,4-Difluoro-phenyl)-4-methyl-5-[1,2,4]triazol-1-ylmethyl-oxazolidin-3-yl]-(4-trifluoromethyl-phenyl)-methanone 

Relevant academic research and scientific papers

NOVEL METHOD FOR PREPARATION OF EPOXYTRIAZOLE DERIVATIVES

The present invention relates to novel processes for preparing epoxytriazole derivatives. The method of claim 1, further comprising the step of adding a base to the intermediate compound. The present invention relates to an epoxytriazole derivative and a manufacturing method thereof. Chemical Formula 1. Here, Ar denotes C. 6 -C10 Aryl group or C aryl group2 -C9 The aryl group 1 -4 is substituted or unsubstituted, and when 2 or more halogen is substituted, the heteroaryl group may be the same as or different from each other, and the heteroaryl group is represented by 1 -4 fluorine, chlorine, or C. 1 -C3 Substituted or unsubstituted alkyl groups, and fluorine, chlorine, or C. 1 -C3 When more than 2 substituents are substituted, each of these substituents may be the same or different and may be different from each other. The A is C. 1 -C3 Represents an alkyl group, and the R represents an alkyl group. 1 And R2 Is a methyl group or an ethyl group.

Discovery of novel indazole-linked triazoles as antifungal agents

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.

ANTIFUNGAL AZOLE DERIVATIVES HAVING A FLUOROVINYL MOIETY AND PROCESS FOR THE PREPARATION THEREOF

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.

Optically active azole derivatives, their production and use

A process for preparing a compound of the formula (IV) or a salt thereof, , wherein R1 is an optionally substituted aliphatic or aromatic hydrocarbon residue or an optionally substituted aromatic heterocyclic group, one of Y and Z is a nitrogen atom and t

Optically active antifungal azoles. I. Synthesis and antifungal activity of (2R,3R)-2-(2,4-difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2- butanol and its stereoisomers

(2R,3R)-2-(2,4-Difluorophenyl)-3-mercapto-1-(1H-1,2,4-triazol-1-yl)-2- butanol [(2R,3R)-7] and its stereoisomers [(2S,3R)-, (2S,3S)- and (2R,3S)-7] were prepared from the optically active oxiranes 6 by a newly developed ring- opening reaction and evaluated for antifungal activity. The thiol (2R,3R)-7 showed extremely potent antifungal activity in vitro and in vivo. The optically active oxirane (2R,3S)-6, a useful intermediate for the synthesis of sulfur-containing antifungal azoles 5, was synthesized from methyl (R)- lactate [(R)-8] via eight steps in a stereocontrolled manner. The key step in the synthesis is the Grignard reaction of an amide derivative [(R)-12a] of (R)-lactic acid with 2,4-difluorophenyl-magnesium bromide (13).

Payne rearrangement route to the optically active oxirane precursor for the preparation of triazole antifungals

Optically active epoxide 1, an important intermediate for the preparation of antifungal triazole-amides 2, was synthesized starting from the (S)-lactic acid-derived ketone 9 and taking advantage of the Payne rearrangement of the epoxyalcohol 8.