This invention discloses an improved process for the preparation of l-(4'-fluorophenyl)-l,3-dihydro-isobenzofiiran-5 carbonitrile of formula-ll, which is useful for the preparation of citalopram of formula-Ill, a well-known antidepressant available in the market. Process for the preparation of compound of formula-II comprises:(i) Reducing the benzophenone derivative of formula-V with sodium borohydride in alcoholic solvent to get the dihydroxy compound of formula-VIII.(ii) Stylizing the dihydroxy compound of formula-VIII with p-toluenesu!fonic acid in toluene to get the phthalate derivative of formula-I.(iii) Reacting the compound of formula I with copper cyanide in dimethylformamide medium to get the Cano derivative of formula-II after re-crystallization from alcoholic solvent with or without dimethylformamide.Compound of formula-II obtained by this method was of high purity and upon further conversion to citalopram product formed in high yield (80%) and high purity (99%).
| # | Name | Date |
|---|---|---|
| 1 | Description_Granted 194522_19-12-2005.pdf | 2005-12-19 |
| 2 | Claims_Granted 194522_19-12-2005.pdf | 2005-12-19 |
| 3 | Abstract_Granted 194522_19-12-2005.pdf | 2005-12-19 |
| 4 | 157m2001.jpg | 2011-09-02 |
| 5 | 0157-mas-2001 petition.pdf | 2011-09-02 |
| 6 | 0157-mas-2001 form-5.pdf | 2011-09-02 |
| 7 | 0157-mas-2001 form-3.pdf | 2011-09-02 |
| 8 | 0157-mas-2001 form-1.pdf | 2011-09-02 |
| 9 | 0157-mas-2001 description (complete).pdf | 2011-09-02 |
| 10 | 0157-mas-2001 description (complete)-duplicate.pdf | 2011-09-02 |
| 11 | 0157-mas-2001 correspondence-po.pdf | 2011-09-02 |
| 12 | 0157-mas-2001 correspondence-others.pdf | 2011-09-02 |
| 13 | 0157-mas-2001 claims.pdf | 2011-09-02 |
| 14 | 0157-mas-2001 claims-duplicate.pdf | 2011-09-02 |
| 15 | 0157-mas-2001 abstract.pdf | 2011-09-02 |
| 16 | 0157-mas-2001 abstract.jpg | 2011-09-02 |
| 17 | 0157-mas-2001 abstract-duplicate.pdf | 2011-09-02 |
| 18 | 157-MAS-2001-RELEVANT DOCUMENTS [14-02-2018(online)].pdf | 2018-02-14 |