WO2024017170A8 - S-(-)-尼古丁(-)-二苯甲酰-l-酒石酸盐晶型、制备方法及应用 - Google Patents

S-(-)-尼古丁(-)-二苯甲酰-l-酒石酸盐晶型、制备方法及应用 Download PDF

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Publication number
WO2024017170A8
WO2024017170A8 PCT/CN2023/107560 CN2023107560W WO2024017170A8 WO 2024017170 A8 WO2024017170 A8 WO 2024017170A8 CN 2023107560 W CN2023107560 W CN 2023107560W WO 2024017170 A8 WO2024017170 A8 WO 2024017170A8
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WO
WIPO (PCT)
Prior art keywords
nicotine
dibenzoyl
crystal form
preparation
tartrate crystal
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PCT/CN2023/107560
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English (en)
French (fr)
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WO2024017170A1 (zh
Inventor
林韶辉
胡永伟
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北京世桥生物制药有限公司
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Application filed by 北京世桥生物制药有限公司 filed Critical 北京世桥生物制药有限公司
Publication of WO2024017170A1 publication Critical patent/WO2024017170A1/zh
Publication of WO2024017170A8 publication Critical patent/WO2024017170A8/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/48—Separation; Purification; Stabilisation; Use of additives
    • C07C67/52—Separation; Purification; Stabilisation; Use of additives by change in the physical state, e.g. crystallisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/78—Benzoic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一种S-(-)-尼古丁(-)-二苯甲酰-L-酒石酸盐晶型、制备方法及应用，所述制备方法包括将S-(-)-尼古丁和(-)-二苯甲酰-L-酒石酸分别溶解于溶剂中，将(-)-二苯甲酰-L-酒石酸溶液加至S-(-)-尼古丁溶液中，搅拌，过滤；将滤饼在一定温度下真空干燥，得到所述S-(-)-尼古丁(-)-二苯甲酰-L-酒石酸盐的晶型。通过X-RPD等检测该盐的晶型，并且将该晶型应用于消旋尼古丁的拆分中，通过控制工艺参数，有效的控制异构体含量，提高拆分效率，实现S-(-)-尼古丁的高效合成。
PCT/CN2023/107560 2022-07-20 2023-07-14 S-(-)-尼古丁(-)-二苯甲酚-l-酒石酸盐晶型、制备方法及应用 WO2024017170A1 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202210860015.X 2022-07-20
CN202210860015.XA CN115093394A (zh) 2022-07-20 2022-07-20 S-(-)-尼古丁(-)-二苯甲酰-l-酒石酸盐晶型、制备方法及应用

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WO2024017170A1 WO2024017170A1 (zh) 2024-01-25
WO2024017170A8 true WO2024017170A8 (zh) 2024-03-14

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WO (1) WO2024017170A1 (zh)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115093394A (zh) * 2022-07-20 2022-09-23 北京世桥生物制药有限公司 S-(-)-尼古丁(-)-二苯甲酰-l-酒石酸盐晶型、制备方法及应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8378111B2 (en) * 2011-02-02 2013-02-19 Divi's Laboratories, Ltd. Process for the resolution of (R,S)-nicotine
US9809567B2 (en) * 2014-12-09 2017-11-07 Njoy, Llc Synthesis and resolution of nicotine
SG11202005641XA (en) * 2017-12-22 2020-07-29 Siegfried Ag Enantiomeric separation of racemic nicotine by addition of an o,o'-disubstituted tartaric acid enantiomer
RU2753548C1 (ru) * 2017-12-22 2021-08-17 Зигфрид АГ Способ производства никотина
CN111004212A (zh) * 2019-12-24 2020-04-14 深圳雾芯科技有限公司 一种制备尼古丁的方法
CN111187250B (zh) * 2020-01-08 2023-04-07 深圳黑尔格科技有限公司 一种拆分式制备光学活性尼古丁的方法
CN113416180A (zh) * 2021-08-09 2021-09-21 东莞市鸿馥生物科技有限公司 一种(s)-1-甲基-2-(3-吡啶基)吡咯烷的拆分方法
CN114249711A (zh) * 2022-03-02 2022-03-29 北京邦克凯姆医药科技有限公司 一种拆分制备尼古丁的方法
CN115093394A (zh) * 2022-07-20 2022-09-23 北京世桥生物制药有限公司 S-(-)-尼古丁(-)-二苯甲酰-l-酒石酸盐晶型、制备方法及应用

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CN115093394A (zh) 2022-09-23
WO2024017170A1 (zh) 2024-01-25

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