Multi-step synthesis of miltefosine: integration of flow chemistry with continuous mechanochemistry
| Title | Multi-step synthesis of miltefosine: integration of flow chemistry with continuous mechanochemistry |
| Publication Type | Journal Article |
| Year of Publication | 2021 |
| Authors | Patil, NB, Atapalkar, RS, Chavan, SP, Kulkarni, AA |
| Journal | Chemistry-A European Journal |
| Volume | 27 |
| Issue | 70 |
| Pagination | 17695-17699 |
| Date Published | DEC |
| Type of Article | Article |
| ISSN | 0947-6539 |
| Keywords | continuous flow, continuous mechanochemistry, miltefosine, multistep synthesis, reactive intermediates |
| Abstract | Herein we report for the first time, an advanced continuous flow synthesis of the blockbuster Leishmaniasis drug miltefosine from simple starting materials by a sequence involving four steps of chemical transformation including a continuous mechanochemical step. First three reaction steps were performed in simple tubular reactors in a telescopic mode, while in the last step the product precipitated from the 3(rd) step was used for a continuous mechanochemical synthesis of miltefosine. When compared to a typical batch protocol that takes 15 h, miltefosine was obtained in 58 % overall yield in flow synthesis mode at the laboratory scale in a total residence time 34 min at synthesis rate of 10 g/hr, which is sufficient to treat 4800 patients per day. |
| DOI | 10.1002/chem.202103499 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 5.236 |
Divison category:
Chemical Engineering & Process Development
Organic Chemistry