CN108137577A - 一种帕博西尼游离碱晶型a和晶型b的制备方法 - Google Patents

一种帕博西尼游离碱晶型a和晶型b的制备方法 Download PDF

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CN108137577A
CN108137577A CN201680054634.2A CN201680054634A CN108137577A CN 108137577 A CN108137577 A CN 108137577A CN 201680054634 A CN201680054634 A CN 201680054634A CN 108137577 A CN108137577 A CN 108137577A
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boxini
water
crystal form
free alkali
preparation
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CN108137577B (zh
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樊海生
郭效文
黄鲁宁
顾虹
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Zhejiang Huahai Pharmaceutical Co Ltd
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Zhejiang Huahai Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/005—Selection of auxiliary, e.g. for control of crystallisation nuclei, of crystal growth, of adherence to walls; Arrangements for introduction thereof
    • B01D9/0054—Use of anti-solvent
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01D—SEPARATION
    • B01D9/00—Crystallisation
    • B01D9/0063—Control or regulation
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本发明公开了一种如式I所示的帕博西尼游离碱晶型A的制备方法，包括以下步骤：在35‑100℃的含水溶剂中将帕博西尼游离碱和/或帕博西尼盐类化合物用无机碱处理得到帕博西尼游离碱晶型A，其中所述含水溶剂为水或水和可与水混溶的有机溶剂的混合溶剂。本发明还公开了一种制备帕博西尼游离碱晶型B的制备方法，包括以下步骤：在0‑20℃的含水溶剂中将帕博西尼盐类化合物用无机碱处理，得到帕博西尼游离碱晶型B，其中所述含水溶剂为水或水和可与水混溶的有机溶剂的混合溶剂。该方法操作安全便捷，污染小，易于工业化生产。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201680054634.2A 2015-11-02 2016-11-02 一种帕博西尼游离碱晶型a和晶型b的制备方法 Active CN108137577B (zh)

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CN2015107335195 2015-11-02
CN201510733519.5A CN106632311B (zh) 2015-11-02 2015-11-02 一种帕博西尼晶型a和晶型b的制备方法
PCT/CN2016/104330 WO2017076288A1 (zh) 2015-11-02 2016-11-02 一种帕博西尼游离碱晶型a和晶型b的制备方法

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Publication number Priority date Publication date Assignee Title
WO2017021111A1 (en) 2015-08-05 2017-02-09 Ratiopharm Gmbh New crystalline form and acetic acid adducts of palbociclib
WO2018009735A1 (en) 2016-07-07 2018-01-11 Plantex Ltd. Solid state forms of palbociclib dimesylate
WO2018073574A1 (en) * 2016-10-20 2018-04-26 Cipla Limited Polymorphic forms of palbociclib
CN108864078B (zh) * 2017-05-10 2021-10-15 江苏豪森药业集团有限公司 帕博西尼晶型b的制备方法
CN109897034A (zh) * 2017-12-07 2019-06-18 南京卡文迪许生物工程技术有限公司 一种高纯度晶型a帕布昔利布及其制备方法和药物组合物
CN108929321A (zh) * 2018-07-03 2018-12-04 威海贯标信息科技有限公司 一种帕博西尼新晶型
CN112462828A (zh) * 2020-10-27 2021-03-09 天津七所高科技有限公司 一种金属脱脂清洗剂游离碱参数自动测量控制方法

Citations (3)

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US7781583B2 (en) * 2006-09-08 2010-08-24 Pfizer Inc Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d] pryimidin-7-ones
CN105008357A (zh) * 2013-02-21 2015-10-28 辉瑞大药厂 选择性cdk4/6抑制剂的固态形式
CN105085517A (zh) * 2015-08-06 2015-11-25 天津华洛康生物科技有限公司 一种结晶型帕博西尼游离碱水合物及其制备方法

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Publication number Priority date Publication date Assignee Title
SI1470124T1 (sl) * 2002-01-22 2006-04-30 Warner Lambert Co 2-(piridin-2-ilamino)-pirido(2,3-d)pirimidin-7-oni
DE102004039083A1 (de) * 2004-08-12 2006-02-23 Degussa Ag Zinnfreie, hochschmelzende Reaktionsprodukte aus carbonylhydrierten Keton-Aldehydharzen, hydrierten Ketonharzen sowie carbonyl- und kernhydrierten Keton-Aldehydharzen auf Basis von aromatischen Ketonen und Polyisocyanten
WO2016024249A1 (en) 2014-08-14 2016-02-18 Sun Pharmaceutical Industries Limited Crystalline forms of palbociclib

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7781583B2 (en) * 2006-09-08 2010-08-24 Pfizer Inc Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d] pryimidin-7-ones
CN105008357A (zh) * 2013-02-21 2015-10-28 辉瑞大药厂 选择性cdk4/6抑制剂的固态形式
CN105085517A (zh) * 2015-08-06 2015-11-25 天津华洛康生物科技有限公司 一种结晶型帕博西尼游离碱水合物及其制备方法

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US20190263809A1 (en) 2019-08-29
WO2017076288A1 (zh) 2017-05-11
US20180319790A1 (en) 2018-11-08
CN108137577B (zh) 2021-04-06
CN106632311B (zh) 2021-05-18
EP3372603A4 (en) 2019-04-24
EP3372603B1 (en) 2022-01-05
EP3372603A1 (en) 2018-09-12
US10766895B2 (en) 2020-09-08
US10329290B2 (en) 2019-06-25
CN106632311A (zh) 2017-05-10

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