Pesticidal compositions and processes related thereto
US-9215870-B2 · Dec 22, 2015 · US
Processes for the preparation of eluxadoline
US10822308B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10822308-B2 |
| Application number | US-201716312401-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 23, 2017 |
| Priority date | Jun 23, 2016 |
| Publication date | Nov 3, 2020 |
| Grant date | Nov 3, 2020 |
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Abstract
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The present invention relates to processes for the preparation of eluxadoline and its intermediates.
First claim
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The invention claimed is: 1. A process for the preparation of a compound of Formula II, comprising cyclizing N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III in the presence of ammonium acetate and toluene, wherein the molar ratio of ammonium acetate to N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III is from 6:1 to 9:1. 2. The process according to claim 1 , wherein the cyclization of N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III to obtain the compound of Formula II is carried out in the presence of acetic acid. 3. The process of claim 2 , wherein the cyclization of N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III is carried out in the presence of acetic acid and the toluene in a ratio of about 1:3 to about 1:8 (vol/vol). 4. The process according to claim 2 , wherein the cyclization of N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III is conducted at a temperature of about 80° C. to about 140° C. 5. The process according to claim 2 , wherein the cyclization of N 2 -[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III proceeds for 2 to 8 hours. 6. The process according to claim 1 , wherein the compound of Formula II is further converted to eluxadoline of Formula I
Assignees
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Classifications
- C07D233/64Primary
with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine · CPC title
Antidiarrhoeals · CPC title
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- What does patent US10822308B2 cover?
- The present invention relates to processes for the preparation of eluxadoline and its intermediates.
- Who is the assignee on this patent?
- Sun Pharmaceutical Ind Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07D233/64. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Nov 03 2020 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).