Abstract: ABSTRACT The present invention relates to novel and improved process for preparing a Azole Antifungal agent or its pharmaceutically acceptable salts. The present invention more " particularly relates to novel and improved process for preparing Luliconazole or its pharmaceutically acceptable salts.
We Claims:
1. An improved process for the preparation of Azole Antifungal Agent of Formula I
or its salts, enantiomers wherein, X] and X2 independently represents hydrogen or halo atom, *represent chiral carbon, which comprises reacting compound of Formula II
or its salts, enantiomers, wherein Xh X2 and * are as defined above, X3 represents leaving group, X4 represents S or O, Ri represents straight or branched alkyl, or cycloalkyl, aryl, alkylaryl, aralkyl, or substituted alkyl, substituted aryl, wherein the substitutions selected from chloro, bromo, fluoro, iodo, nitro, carbonyl, carboxylic acids, with compound of Formula in
ether, tetrahydrofuran and dimethoxyethane, methanol, ethanol, n-propanol, isopropanol, n-butanol and t-butanol, methylene chloride, ethylene dichloride, carbon tetra chloride, chloroform, chloro benzene, benzene, toluene, xylene, heptane, hexane, cyclohexane, acetone, ethyl methyl ketone, diethyl ketone, methyl tert-butyl ketone, isopropyl ketone, ethyl acetate, methyl acetate, n-butyl acetate, isobutyl acetate, sec -butyl acetate, isopropyl acetate and their mixtures thereof.
3. An improved process for the preparation of Luliconazole of Formula IA
which comprises reacting compound of Formula HA
with compound of Formula IHA
or its salts, which comprises reacting compound of Formula HE
wherein X3 represents a leaving group, m represents 0 to 3, Y represents substituents selected from halo or carboxylic acids, with compound of Formula III
wherein M represents hydrogen or alkali metal salts to give Lanoconazole of Formula (IB).
6. Crystalline Form-S of compound of Formula IIA characterized by an X-ray powder diffraction (XRPD) spectrum having peaks at 12.3, 12.6, 25.3, 26.2 ±0.2 degrees of 28.
7. Process for the preparation of crystalline Form-S of Formula DA
characterized by an X-ray powder diffraction (XRPD) spectrum having peaks at 12.3, 12.6, 25.3, 26.2 ±0.2 degrees of 26, which comprises
a) dissolving crude compound of Formula IIA in a solvent selected from ketones and alcohols,
b) adding anti-solvent to the step a) solution,
c) isolating crystalline Form-S of compound of Formula IIA.
| # | Name | Date |
|---|---|---|
| 1 | Abstract_As Filed_25-01-2018.pdf | 2018-01-25 |
| 1 | Form2 Title Page_Provisional_30-01-2017.pdf | 2017-01-30 |
| 2 | Claims_As Filed_25-01-2018.pdf | 2018-01-25 |
| 2 | Form1_As Filed_30-01-2017.pdf | 2017-01-30 |
| 3 | Drawing_As Filed_30-01-2017.pdf | 2017-01-30 |
| 3 | Correspondence by Applicant_Submission of Document_25-01-2018.pdf | 2018-01-25 |
| 4 | Description Provisional_As Filed_30-01-2017.pdf | 2017-01-30 |
| 4 | Description Complete_As Filed_25-01-2018.pdf | 2018-01-25 |
| 5 | Correspondence by Applicant_Provisional Application_30-01-2017.pdf | 2017-01-30 |
| 5 | Form2 Title Page_Complete_25-01-2018.pdf | 2018-01-25 |
| 6 | Form3_As Filed_25-01-2018.pdf | 2018-01-25 |
| 7 | Correspondence by Applicant_Provisional Application_30-01-2017.pdf | 2017-01-30 |
| 7 | Form2 Title Page_Complete_25-01-2018.pdf | 2018-01-25 |
| 8 | Description Complete_As Filed_25-01-2018.pdf | 2018-01-25 |
| 8 | Description Provisional_As Filed_30-01-2017.pdf | 2017-01-30 |
| 9 | Correspondence by Applicant_Submission of Document_25-01-2018.pdf | 2018-01-25 |
| 9 | Drawing_As Filed_30-01-2017.pdf | 2017-01-30 |
| 10 | Form1_As Filed_30-01-2017.pdf | 2017-01-30 |
| 10 | Claims_As Filed_25-01-2018.pdf | 2018-01-25 |
| 11 | Form2 Title Page_Provisional_30-01-2017.pdf | 2017-01-30 |
| 11 | Abstract_As Filed_25-01-2018.pdf | 2018-01-25 |