Abstract: 1. A process for the preparation of Anidulafungin which comprising the following steps; a) treating 4"-(Pentyloxy)-l, r:4",l"-terphenyl-4-carboxylic acid with 2-Chloro-4,6-dimethoxy-l,3,5-triazine (CDMT) in a solvent with base to prepare compound of Formula II; (2-({[4"-(Pentyloxy)-l, l":4",l"-terphenyl-4-yl]carbonyl}oxy)-4,6-dimethoxy-1,3,5-triazine) b) reacting the compound of Formula II of step (a) with Echinocandin B in a mixture of solvent and base to obtain Anidulafungin, wherein the said Echinocandin B is in hydrochloride form; c) reacting the compound of Formula II of step (a) with Echinocandin B in a mixture of solvent to obtained Anidulafungin, wherein the said Echinocandin B is in base form; d) purifying the product obtained in step (b) & step (c) using protic solvents containing fructose.
We claim,
1. A process for the preparation of Anidulafungin which comprising the following steps;
a) treating 4"-(Pentyloxy)-l, r:4',l"-terphenyl-4-carboxylic acid with 2-Chloro-4,6-dimethoxy-l,3,5-triazine (CDMT) in a solvent with base to prepare compound of Formula II; (2-({[4"-(Pentyloxy)-l, l':4',l"-terphenyl-4-yl]carbonyl}oxy)-4,6-dimethoxy-1,3,5-triazine)
b) reacting the compound of Formula II of step (a) with Echinocandin B in a mixture of solvent and base to obtain Anidulafungin, wherein the said Echinocandin B is in hydrochloride form;
c) reacting the compound of Formula II of step (a) with Echinocandin B in a mixture of solvent to obtained Anidulafungin, wherein the said Echinocandin B is in base form;
d) purifying the product obtained in step (b) & step (c) using protic solvents containing fructose.
2. Compound of Formula II (2-({ [4"-(Pentyloxy)-1, 1 *:4', 1 "-terphenyl-4-
yl]carbonyl}oxy)-4,6-dimethoxy-l,3,5-triazine)
The process as claimed in claim 1, wherein the solvent used in step (a) is Dimethyl sulphoxide, N, N-Dimethyl formamide and most preferably N, N-Dimethyl formamide.
The process as claimed in claim 1, wherein the base used in step (a) is Triethylamine, Diisopropyl ethylamine and N-methyl morpholine, preferably triethylamine and most preferably N-methyl morpholine.
The process as claimed in claim 1, wherein the temperature of the reaction in step (a) is between 10° and 40°C and preferably between 20°C and 30°C and most preferably between 25°C and 30°C.
The process as claimed in claim 1, wherein duration of the reaction in step (a) is between 1 and 5hrs and preferably between 2 and 4 hrs and most preferably between 2 and 3 hrs.
The process as claimed in claim 1, wherein reacting the compound of Formula II of step (a) with Echinocandin B hydrochloride in N,N-Dimethyl formamide(DMF), N-Methyl morpholine (NMM), toluene or mixture thereof at the temperature between 30-40°C to obtain Anidulafungin.
The process as claimed in claim 1, wherein the solvent used in the Step (b) & (c) is N,N-Dimethyl formamide(DMF), toluene, Tetrahydrofuran, more preferably DMF and toluene.
The process as claimed in claim 1, wherein the temperature of the reaction in step (b) & (c) is between 10° and 50°C and preferably between 20°C and 40°C and most preferably between 30°C and 40°C.
). The process as claimed in claim 1, wherein duration of the reaction in step (b) & (c) is between 2 and lOhrs and preferably between 4 and 8 hrs and most preferably between 3 and 6 hrs.
[. The process as claimed in claim 1, wherein the protic solvent used in step (d) is methanol, ethanol, propanol, isopropanol or mixture thereof; preferably methanol, ethanol or mixture thereof; most preferably ethanol.
| # | Name | Date |
|---|---|---|
| 1 | 5273-CHE-2012 CORRESPONDENCE OTHERS 17-12-2012.pdf | 2012-12-17 |
| 2 | 5273-CHE-2012 FORM-2 17-12-2012.pdf | 2012-12-17 |
| 3 | 5273-CHE-2012 FORM-1 17-12-2012.pdf | 2012-12-17 |
| 4 | 5273-CHE-2012 CORRESPONDENCE OTHERS 26-12-2012.pdf | 2012-12-26 |
| 5 | 5273-CHE-2012 FORM-18 26-12-2012.pdf | 2012-12-26 |
| 6 | 5273-CHE-2012 Description(Complete).pdf | 2016-12-29 |
| 7 | 5273-CHE-2012 Claims.pdf | 2016-12-29 |
| 8 | 5273-CHE-2012-FER.pdf | 2017-06-20 |
| 9 | Correspondence by agent_Reply to Examination Report_18-09-2017.pdf | 2017-09-18 |
| 10 | Abstract_After Filing_18-09-2017.pdf | 2017-09-18 |
| 11 | 5273-CHE-2012-HearingNoticeLetter.pdf | 2017-10-28 |
| 12 | Correspondence by Applicant_Reply to Hearing_03-11-2017.pdf | 2017-11-03 |
| 13 | Abstract_Hearing Reply_03-11-2017.pdf | 2017-11-03 |
| 14 | Petition under rule137_Form3_13-11-2017.pdf | 2017-11-13 |
| 15 | Form3_Proof of Right_13-11-2017.pdf | 2017-11-13 |
| 16 | Correspondence by Applicant_Petition under rule137_13-11-2017.pdf | 2017-11-13 |
| 17 | Abstract_After Filing_13-11-2017.pdf | 2017-11-13 |
| 18 | Description_Granted 289731_20-11-2017.pdf | 2017-11-20 |
| 19 | Claims_Granted 289731_20-11-2017.pdf | 2017-11-20 |
| 20 | Abstract_Granted 289731_20-11-2017.pdf | 2017-11-20 |
| 21 | 5273-CHE-2012-PatentCertificate20-11-2017.pdf | 2017-11-20 |
| 22 | 5273-CHE-2012-IntimationOfGrant20-11-2017.pdf | 2017-11-20 |
| 23 | Correspondence by Applicant_Renewal Fees_19-01-2018.pdf | 2018-01-19 |
| 24 | Form-27_Statement Of Working_26-03-2018.pdf | 2018-03-26 |
| 25 | Form 27_License_27-03-2019.pdf | 2019-03-27 |
| 26 | 5273-CHE-2012_Form27 License_23-03-2020.pdf | 2020-03-23 |
| 27 | 5273-CHE-2012-Form13_Address of service Change_22-10-2020.pdf | 2020-10-22 |
| 28 | 5273-CHE-2012-Correspondence-01-12-2020.pdf | 2020-12-01 |
| 29 | 5273-CHE-2012-Form 27_Statement of Working_13-10-2021.pdf | 2021-10-13 |
| 30 | 5273-CHE-2012_Renewal Fee_29-10-2021.pdf | 2021-10-29 |
| 31 | 5273-CHE-2012-Form 27_Statement of Working_02-09-2022.pdf | 2022-09-02 |
| 32 | 289731-Form30_Renewal Fees_25-10-2022.pdf | 2022-10-25 |
| 33 | 5273-CHE-2012-RELEVANT DOCUMENTS [13-03-2024(online)].pdf | 2024-03-13 |
| 1 | SEARCHSTRATEGY_14-06-2017.pdf |