CN115103836A - 制备手性苯并二氮杂卓酮衍生物的方法 - Google Patents

制备手性苯并二氮杂卓酮衍生物的方法 Download PDF

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Publication number
CN115103836A
CN115103836A CN202180014113.5A CN202180014113A CN115103836A CN 115103836 A CN115103836 A CN 115103836A CN 202180014113 A CN202180014113 A CN 202180014113A CN 115103836 A CN115103836 A CN 115103836A
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compound
formula
solvent
combination
represented
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CN202180014113.5A
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Chinese (zh)
Inventor
克里斯多佛·M·西马鲁斯蒂
阿南德库马尔·马丹拉尔·拉赫蒂
马丹·拉贾·戈帕尔·雷迪·德拉姆
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Yimi Rumei Co ltd
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Ayala Pharmaceuticals Inc
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Publication of CN115103836A publication Critical patent/CN115103836A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/282-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • C07D243/26Preparation from compounds already containing the benzodiazepine skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • C07D243/30Preparation including building-up the benzodiazepine skeleton from compounds already containing hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202180014113.5A 2020-02-16 2021-02-16 制备手性苯并二氮杂卓酮衍生物的方法 Pending CN115103836A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062977316P 2020-02-16 2020-02-16
US62/977,316 2020-02-16
PCT/US2021/018137 WO2021163676A1 (en) 2020-02-16 2021-02-16 Methods of preparing chiral benzodiazepinone derivatives

Publications (1)

Publication Number Publication Date
CN115103836A true CN115103836A (zh) 2022-09-23

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CN202180014113.5A Pending CN115103836A (zh) 2020-02-16 2021-02-16 制备手性苯并二氮杂卓酮衍生物的方法

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US (2) US12503449B2 (https=)
EP (1) EP4107148A4 (https=)
JP (1) JP2023513731A (https=)
KR (1) KR20220143094A (https=)
CN (1) CN115103836A (https=)
AU (1) AU2021218456A1 (https=)
BR (1) BR112022016249A2 (https=)
CA (1) CA3171651A1 (https=)
IL (1) IL295572A (https=)
MX (1) MX2022010079A (https=)
WO (1) WO2021163676A1 (https=)

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0253571A1 (en) * 1986-07-14 1988-01-20 Merck & Co. Inc. Process for resolution and race mization of amines with acidic alpha-hydrogens
WO2010073253A1 (en) * 2008-12-22 2010-07-01 Natco Pharma Limited Method for preparing an optically active frovatriptan
US20150045575A1 (en) * 2012-03-30 2015-02-12 Merck Sharp & Dohme Corp. Process for preparing fluoroleucine alkyl esters
CN104822677A (zh) * 2012-09-21 2015-08-05 百时美施贵宝公司 氟烷基-1,4-苯并二氮杂*酮化合物
CN105308030A (zh) * 2012-09-21 2016-02-03 百时美施贵宝公司 烷基、氟烷基-1,4-苯并二氮杂*酮化合物
CN105439939A (zh) * 2015-11-12 2016-03-30 四川恒康科技发展有限公司 一种(S)-N-Boc-3-羟基哌啶的合成方法
CN106660949A (zh) * 2015-02-17 2017-05-10 株式会社爱茉莉太平洋 N‑[4‑(1‑氨基乙基)‑苯基]‑磺酰胺衍生物的手性拆分方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL9000386A (nl) * 1990-02-16 1991-09-16 Stamicarbon Werkwijze voor de bereiding van optisch aktief aminozuuramide.
JPH0751555B2 (ja) 1992-04-15 1995-06-05 キヤノン株式会社 ジイモニウム塩化合物
BRPI0520554A2 (pt) * 2005-09-19 2009-06-13 Arrow Therapeutics Ltd uso de uma benzodiazepina ou um sal farmaceuticamente aceitável do mesmo, método para tratar ou prevenir uma infecção por hcv em um paciente, derivado de benzodiazepina ou um sal famaceuticamente aceitável do mesmo, e, composição farmacêutica
EP2897942B1 (en) 2012-09-21 2016-08-31 Bristol-Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch inhibitors
TWI614238B (zh) * 2012-09-21 2018-02-11 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯并二氮呯酮化合物及其前藥

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0253571A1 (en) * 1986-07-14 1988-01-20 Merck & Co. Inc. Process for resolution and race mization of amines with acidic alpha-hydrogens
WO2010073253A1 (en) * 2008-12-22 2010-07-01 Natco Pharma Limited Method for preparing an optically active frovatriptan
US20150045575A1 (en) * 2012-03-30 2015-02-12 Merck Sharp & Dohme Corp. Process for preparing fluoroleucine alkyl esters
CN104822677A (zh) * 2012-09-21 2015-08-05 百时美施贵宝公司 氟烷基-1,4-苯并二氮杂*酮化合物
CN105308030A (zh) * 2012-09-21 2016-02-03 百时美施贵宝公司 烷基、氟烷基-1,4-苯并二氮杂*酮化合物
CN106660949A (zh) * 2015-02-17 2017-05-10 株式会社爱茉莉太平洋 N‑[4‑(1‑氨基乙基)‑苯基]‑磺酰胺衍生物的手性拆分方法
CN105439939A (zh) * 2015-11-12 2016-03-30 四川恒康科技发展有限公司 一种(S)-N-Boc-3-羟基哌啶的合成方法

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MX2022010079A (es) 2022-09-02
US20250346565A1 (en) 2025-11-13
BR112022016249A2 (pt) 2022-10-11
CA3171651A1 (en) 2021-08-19
EP4107148A1 (en) 2022-12-28
WO2021163676A1 (en) 2021-08-19
EP4107148A4 (en) 2024-05-15
IL295572A (en) 2022-10-01
US20230108536A1 (en) 2023-04-06
US12503449B2 (en) 2025-12-23
AU2021218456A1 (en) 2022-09-22
KR20220143094A (ko) 2022-10-24
JP2023513731A (ja) 2023-04-03

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Effective date of registration: 20251110

Address after: Washington State

Applicant after: Yimi Rumei Co.,Ltd.

Country or region after: U.S.A.

Address before: Delaware, USA

Applicant before: Ayala pharmaceutical Co.

Country or region before: U.S.A.