CN117715889A - 制备双官能化合物的方法 - Google Patents

制备双官能化合物的方法 Download PDF

Info

Publication number
CN117715889A
CN117715889A CN202280052419.4A CN202280052419A CN117715889A CN 117715889 A CN117715889 A CN 117715889A CN 202280052419 A CN202280052419 A CN 202280052419A CN 117715889 A CN117715889 A CN 117715889A
Authority
CN
China
Prior art keywords
solvent
solution
reaction mixture
temperature
mixture
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202280052419.4A
Other languages
English (en)
Chinese (zh)
Inventor
C·H·陈
H·董
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Arvinas Inc
Original Assignee
Arvinas Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Arvinas Inc filed Critical Arvinas Inc
Publication of CN117715889A publication Critical patent/CN117715889A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J25/00—Catalysts of the Raney type
    • B01J25/02—Raney nickel
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/19—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Health & Medical Sciences (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
CN202280052419.4A 2021-07-26 2022-07-26 制备双官能化合物的方法 Pending CN117715889A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163225858P 2021-07-26 2021-07-26
US63/225,858 2021-07-26
PCT/US2022/038343 WO2023009521A1 (en) 2021-07-26 2022-07-26 Methods of manufacturing a bifunctional compound

Publications (1)

Publication Number Publication Date
CN117715889A true CN117715889A (zh) 2024-03-15

Family

ID=83508570

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280052419.4A Pending CN117715889A (zh) 2021-07-26 2022-07-26 制备双官能化合物的方法

Country Status (10)

Country Link
US (2) US12286419B2 (https=)
EP (1) EP4377296A1 (https=)
JP (1) JP2024527934A (https=)
KR (1) KR20240040769A (https=)
CN (1) CN117715889A (https=)
AU (1) AU2022319702A1 (https=)
CA (1) CA3227425A1 (https=)
IL (1) IL309839A (https=)
MX (1) MX2024001118A (https=)
WO (1) WO2023009521A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
KR20220054347A (ko) 2019-08-26 2022-05-02 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 유도체로 유방암을 치료하는 방법
CA3227425A1 (en) 2021-07-26 2023-02-02 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound
WO2025245032A1 (en) 2024-05-20 2025-11-27 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound
WO2026018182A1 (en) 2024-07-19 2026-01-22 Pfizer Inc. Process for preparing a cis-1,2-diaryltetralin derivative

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4885363A (en) 1987-04-24 1989-12-05 E. R. Squibb & Sons, Inc. 1-substituted-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs
MX174467B (es) 1986-01-23 1994-05-17 Squibb & Sons Inc 1,4,7-triscarboximetil-1,4,7,10-tetraazaciclodo decano substituido en 1 y compuestos analogos
US5965107A (en) 1992-03-13 1999-10-12 Diatide, Inc. Technetium-99m labeled peptides for imaging
US5808091A (en) 1991-10-29 1998-09-15 Bracco International B.V. Rhenium and technetium complexes containing a hypoxia localizing moiety
US5608110A (en) 1993-06-15 1997-03-04 Bracco International B.V. Heteroatom-bearing ligands and metal complexes thereof
ES2114209T3 (es) 1993-07-19 1998-05-16 Resolution Pharm Inc Queladores de radionuclidos de tipo hidrazino que tienen una configuracion n3s.
US5574140A (en) 1993-09-03 1996-11-12 Resolution Pharmaceutical Inc. Hydrazino-type N2 S2 chelators
US5662885A (en) 1994-07-22 1997-09-02 Resolution Pharmaceuticals Inc. Peptide derived radionuclide chelators
US6093382A (en) 1998-05-16 2000-07-25 Bracco Research Usa Inc. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
ES2885769T3 (es) * 2012-08-09 2021-12-15 Celgene Corp Una forma sólida de clorhidrato de (s)-3-(4-((4-morpholinometil)bencil)oxi)-1-oxoisoindolin-2-il)piperidina-2,6-diona
BR112019011200B1 (pt) 2016-12-01 2021-12-28 Arvinas Operations, Inc Derivados de tetrahidronaftaleno e tetrahidroisoquinolina como degradadores do receptor de estrogênio
EP4406609A3 (en) 2017-05-30 2024-10-02 Day One Biopharmaceuticals, Inc. Method for producing optically active compound
EP3412666A1 (en) * 2017-06-07 2018-12-12 Albany Molecular Research, Inc. Process and intermediates for the preparation of bcl-2 inhibitors including venetoclax through reductive amination
US10717703B2 (en) * 2017-08-21 2020-07-21 Celgene Corporation Processes for the preparation of (S)-tert-butyl 4,5-diamino-5-oxopentanoate
IL302595A (en) * 2018-04-13 2023-07-01 Arvinas Operations Inc Servalon ligands and bifunctional compounds containing them
JP7307796B2 (ja) 2019-09-23 2023-07-12 アキュター バイオテクノロジー インコーポレイテッド アンドロゲン受容体分解活性を有する新規の置換キノリン－８－カルボニトリル誘導体およびその使用
EP3835298B1 (en) 2019-12-12 2024-06-26 Accutar Biotechnology Inc. Novel chroman derivatives having estrogen receptor degradation activity and uses thereof
CA3227425A1 (en) 2021-07-26 2023-02-02 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound
CN113816927B (zh) 2021-11-23 2022-02-25 苏州国匡医药科技有限公司 一种arv-471中间体的制备方法
CN117126133A (zh) 2023-08-14 2023-11-28 中国海洋大学 一种化合物及其用途

Also Published As

Publication number Publication date
MX2024001118A (es) 2024-04-10
EP4377296A1 (en) 2024-06-05
JP2024527934A (ja) 2024-07-26
US20250326740A1 (en) 2025-10-23
IL309839A (en) 2024-02-01
WO2023009521A1 (en) 2023-02-02
KR20240040769A (ko) 2024-03-28
CA3227425A1 (en) 2023-02-02
US20230069491A1 (en) 2023-03-02
US12286419B2 (en) 2025-04-29
AU2022319702A1 (en) 2024-02-15

Similar Documents

Publication Publication Date Title
CN117715889A (zh) 制备双官能化合物的方法
WO2018175927A2 (en) Peptide nucleic acid (pna) monomers with an orthogonally protected ester moiety
KR100655104B1 (ko) Ｌ-페닐에프린 하이드로클로라이드의 제조방법
US20150353577A1 (en) Method for producing (1s,4s,5s)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one
EP2407468A2 (en) Improved method for preparing meropenem using zinc powder
CA3006537A1 (en) Process for preparation of lisdexamphetamine
CN120271577A (zh) 一种alk抑制剂化合物及其中间体的制备方法
CN1990455B (zh) 一种简单、新颖的茚衍生物的制备方法
CN107216332B (zh) 叔丁基-7-羟甲基-7,8-二氢4h吡唑并二氮杂卓5(6h)甲酸基酯的合成方法
WO2024015861A1 (en) Methods of preparation of heterocyclic compounds
JP5166747B2 (ja) アルキルアミノピリジン類の精製方法
CN106478484B (zh) 一种制备阿莫曲坦关键中间体的方法
CN108101841A (zh) 一种制备茚达特罗或其盐的方法
JPH03112998A (ja) アミカシンの製造方法
CN108147988B (zh) 一种高手性纯度内酰胺化合物的制备方法
CN119684305B (zh) 一种8,8-二氟-2,6-二氮杂螺[3.4]辛烷类化合物的制备方法
JP5397706B2 (ja) 高純度１−ベンジル−３−アミノピロリジンの製造方法
US10207986B2 (en) Method for preparing D-arginine
CN110627768A (zh) 一种莫西沙星降解杂质j的制备方法
CN117105840A (zh) 制备手性内酰胺衍生物的方法
CZ282398B6 (cs) Způsob výroby 1-R1-3-R2-tricyklo(3,3,1,1,3,7)decyl-5-aminu
CN112679506A (zh) 一种枸橼酸托法替布的制备方法
CN121449621A (zh) 一种高纯度甲苯磺酸利特昔替尼中间体的制备方法
CN112266348A (zh) 一种l-脯氨酰胺的制备方法
CN112062754A (zh) 一种合成Dorzagliatin的中间体的制备方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination