(ppm): 9.04 (1H), 8.84 (1H), 8.23 (1H),
7.61 (1H),
7.28 (1H),
7.17 (1H),
6.91 (1H),
5.97 (1H),
4.80 (1H),
4.34 (1H),
3.93 (1H),
1.1 (3H)………….US8263769
13 C NMR
DMSO-d6
HPLC
| Cited Patent | Filing date | Publication date | Applicant | Title |
|---|---|---|---|---|
| US6586594 | 26 Jul 1996 | 1 Jul 2003 | Pfizer, Inc. | Preparation of triazoles by organometallic addition to ketones and intermediates therefor |
| CN1488630A | 8 Oct 2002 | 14 Apr 2004 | 张文更 | Method for preparing triazole antifungal agent |
| CN1814597A | 9 Dec 2005 | 9 Aug 2006 | 北京丰德医药科技有限公司 | New method for preparing voriconazole |
| EP0440372A1 | 24 Jan 1991 | 7 Aug 1991 | Pfizer Limited | Triazole antifungal agents |
| GB2452049A | Title not available | |||
| WO1993007139A1 | 1 Oct 1992 | 15 Apr 1993 | Pfizer Ltd | Triazole antifungal agents |
| WO1997006160A1 | 26 Jul 1996 | 20 Feb 1997 | Michael Butters | Preparation of triazoles by organometallic addition to ketones and intermediates therefor |
| WO2006065726A2 | 13 Dec 2005 | 22 Jun 2006 | Reddys Lab Ltd Dr | Process for preparing voriconazole |
| WO2007013096A1 | 26 Jun 2006 | 1 Feb 2007 | Msn Lab Ltd | Improved process for the preparation of 2r, 3s-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl) butan-2-ol (voriconazole) |
| WO2007132354A2 | 29 Jan 2007 | 22 Nov 2007 | Medichem Sa | Process for preparing voriconazole, new polymorphic form of intermediate thereof, and uses thereof |
| WO2009024214A1 * | 10 Jul 2008 | 26 Feb 2009 | Axellia Pharmaceuticals Aps | Process for the production of voriconazole |
| WO2009084029A2 | 2 Dec 2008 | 9 Jul 2009 | Venkatesh Bhingolikar | Improved process for the preparation of (2r,3s)-2-(2,4- difluqrophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl) butan-2-ol |
| US8575344 * | 1 Feb 2011 | 5 Nov 2013 | Dongkook Pharmaceutical Co., Ltd. | Process for preparing voriconazole by using new intermediates |
| US20130005973 * | 1 Feb 2011 | 3 Jan 2013 | Dongkook Pharmaceutical Co., Ltd. | Process for preparing voriconazole by using new intermediates |
Reference |
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | Butters et al., “Process Development of Voriconazole: A Novel Broad-Spectrum Triazole Antifungal Agent,” Organic Process Research & Development, 2001, vol. 5, pp. 28-36. | ||||||||||||||||||||||||||||||||||||
MOLFILE
COPY ONLY BLUE SECTION
START
64684.mol
ChemDraw07261512442D
26 28 0 0 0 0 0 0 0 0999 V2000
0.5118 1.1267 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-0.2030 0.7149 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-0.9179 0.3031 0.0000 H 0 0 0 0 0 0 0 0 0 0 0 0
-0.6206 1.4298 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-0.2030 2.1447 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
-0.6206 2.8595 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-1.4441 2.8595 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
-1.8559 2.1447 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-1.4441 1.4298 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-1.8559 0.7149 0.0000 F 0 0 0 0 0 0 0 0 0 0 0 0
0.2088 0.0000 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
-0.5062 -0.4117 0.0000 O 0 0 0 0 0 0 0 0 0 0 0 0
0.9236 0.4118 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
0.9236 1.2411 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
1.5928 1.7215 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
1.3354 2.5107 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
0.5118 2.5107 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
0.2545 1.7215 0.0000 N 0 0 0 0 0 0 0 0 0 0 0 0
0.6205 -0.7149 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
0.2088 -1.4297 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
0.6205 -2.1446 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
1.4440 -2.1446 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
1.8559 -2.8595 0.0000 F 0 0 0 0 0 0 0 0 0 0 0 0
1.8559 -1.4297 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
1.4440 -0.7149 0.0000 C 0 0 0 0 0 0 0 0 0 0 0 0
1.8559 0.0000 0.0000 F 0 0 0 0 0 0 0 0 0 0 0 0
1 2 1 0
2 3 1 1
2 4 1 0
2 11 1 0
4 5 1 0
4 9 2 0
5 6 2 0
6 7 1 0
7 8 2 0
8 9 1 0
9 10 1 0
11 12 1 1
11 13 1 0
11 19 1 0
13 14 1 0
14 15 1 0
14 18 1 0
15 16 2 0
16 17 1 0
17 18 2 0
19 20 1 0
19 25 2 0
20 21 2 0
21 22 1 0
22 23 1 0
22 24 2 0
24 25 1 0
25 26 1 0
M END
END
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Filed under: Uncategorized Tagged: VORICONAZOLE
