(EP3302473) Preparation of sufentanil citrate and sufentanil base 机翻标题: 暂无翻译,请尝试点击翻译按钮。

源语言标题
(EP3302473) Preparation of sufentanil citrate and sufentanil base
公开号/公开日
EP3302473EP3302473EP3302473 / 2020-07-082019-04-172018-04-11
申请号/申请日
EP16800663 / 2016-05-25
发明人
KLEMM GEORGE HELMUTORR BRIANMCCLENAGHAN JOEL;
申请人
SPECGX;
主分类号
IPC分类号
A61K-031/4535 C07C-051/41 C07D-401/06 C07D-409/06
摘要
(EP3302473) Provided herein are processes for forming sufentanil citrate from sufentanil base. One process comprises forming sufentanil citrate in the presence of a polar non-aqueous solvent. Other processes comprise forming sufentanil citrate in the presence of water.
机翻摘要
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地址
代理人
(EP3302473) Jones, Nicholas Andrew ; Withers & Rogers LLP ([GB]) Reg. Nb: 100055529
代理机构
;
优先权号
2015US-62166911 2016WO-US34091
主权利要求
(EP3302473) 1. A process for forming sufentanil citrate from sufentanil base, the process comprising :   (a) contacting sufentanil base with a polar non-aqueous solvent to form a mixture, wherein the volume to mass ratio (mL:g) of the polar non-aqueous solvent to sufentanil base is from 2:1 to 12:1 and the contacting occurs at a temperature from 70°C to 90°C;   (b) contacting the mixture with citric acid to form a sufentanil citrate mixture, wherein the contacting occurs at a temperature from 70°C to 90°C and the sufentanil citrate mixture is free of an oil phase;   (c) cooling the sufentanil citrate mixture to a temperature from 50°C to 60°C to form solid sufentanil citrate; and   (d) recovering sufentanil citrate at a temperature from 50°C to 60°C. 2. The process of claim 1, wherein the polar non-aqueous solvent is ethyl acetate, isopropyl acetate, methyl isobutyl ketone, methyl ethyl ketone, or C1-C5 alcohol. 3. The process of of either claim 1 or claim 2, wherein the polar non-aqueous solvent is isopropyl alcohol; and the volume to mass ratio (mL:g) of the polar non-aqueous solvent to sufentanil base is from 4:1 to 8:1. 4. The process of any one of claims 1 to 3, wherein step (c) further comprises seeding the sufentanil citrate mixture with crystals of sufentanil citrate, to form solid sufentanil citrate. 5. The process of any one of claims 1 to 4, wherein step (d) comprises filtration. 6. The process of any one of claims 1 to 5, wherein the solid sufentanil citrate recovered at step (d) contains less than 5000 ppm of the polar non-aqueous solvent. 7. The process of any one of claims 1 to 6, wherein the solid sufentanil citrate recovered at step (d) contains less than 2000 ppm of the polar non-aqueous solvent. 8. The process of any one of claims 1 to 7, further comprising:   (i) contacting the mixture remaining after recovery of solid sufentanil citrate with a proton acceptor to form a sufentanil base mixture;   (ii) cooling the sufentanil base mixture to form solid sufentanil base; and   (iii) recovering solid sufentanil base. 9. The process of claim 8, wherein the proton acceptor is a hydroxide salt. 10. The process of claim 8 or claim 9, further comprising contacting solid sufentanil base with a non-polar solvent to form crystalline sufentanil base. 11. The process of claim 10, wherein the non-polar solvent is an alkane.
法律状态
GRANTED
专利类型码
B1A4A1
国别省市代码
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