CN111886235B - 用于制备曲唑酮的连续方法 - Google Patents

用于制备曲唑酮的连续方法 Download PDF

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Publication number
CN111886235B
CN111886235B CN201980011910.0A CN201980011910A CN111886235B CN 111886235 B CN111886235 B CN 111886235B CN 201980011910 A CN201980011910 A CN 201980011910A CN 111886235 B CN111886235 B CN 111886235B
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chlorophenyl
piperazine
trazodone
flow reactor
continuously
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Chinese (zh)
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CN111886235A (zh
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T·伊亚克安格利
L·M·莫罗
G·卡拉希奥罗托里希阿洛罗
C·卡瓦利斯奇亚
G·弗尔罗逖
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Angelini Acraf SpA
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Aziende Chimiche Riunite Angelini Francesco ACRAF SpA
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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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • 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
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/0093—Microreactors, e.g. miniaturised or microfabricated reactors
    • 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
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/18—Stationary reactors having moving elements inside
    • 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
    • B01J14/00—Chemical processes in general for reacting liquids with liquids; Apparatus specially adapted therefor
    • 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
    • B01J2204/00—Aspects relating to feed or outlet devices; Regulating devices for feed or outlet devices
    • B01J2204/007—Aspects relating to the heat-exchange of the feed or outlet devices
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002—Chemical plants
    • B01J2219/00027—Process aspects
    • B01J2219/00029—Batch processes
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002—Chemical plants
    • B01J2219/00027—Process aspects
    • B01J2219/00033—Continuous processes
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00788—Three-dimensional assemblies, i.e. the reactor comprising a form other than a stack of plates
    • B01J2219/00792—One or more tube-shaped elements
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00801—Means to assemble
    • B01J2219/0081—Plurality of modules
    • B01J2219/00813—Fluidic connections
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00851—Additional features
    • B01J2219/00867—Microreactors placed in series, on the same or on different supports
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00851—Additional features
    • B01J2219/00869—Microreactors placed in parallel, on the same or on different supports
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00851—Additional features
    • B01J2219/00871—Modular assembly
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00781—Aspects relating to microreactors
    • B01J2219/00873—Heat exchange
    • 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
    • B01J8/00—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes
    • B01J8/02—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes with stationary particles, e.g. in fixed beds
    • B01J8/0292—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes with stationary particles, e.g. in fixed beds with stationary packing material in the bed, e.g. bricks, wire rings, baffles
    • 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
    • B01J8/00—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes
    • B01J8/18—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes with fluidised particles
    • B01J8/24—Chemical or physical processes in general, conducted in the presence of fluids and solid particles; Apparatus for such processes with fluidised particles according to "fluidised-bed" technique

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Combustion & Propulsion (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201980011910.0A 2018-02-07 2019-02-05 用于制备曲唑酮的连续方法 Active CN111886235B (zh)

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Application Number Priority Date Filing Date Title
EP18155470 2018-02-07
EP18155470.0 2018-02-07
PCT/EP2019/052690 WO2019154770A1 (en) 2018-02-07 2019-02-05 Continuous process for the preparation of trazodone

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CN111886235A CN111886235A (zh) 2020-11-03
CN111886235B true CN111886235B (zh) 2023-06-30

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Publication number Priority date Publication date Assignee Title
CN116253696A (zh) * 2021-12-10 2023-06-13 安徽省化工研究院 一种噁草酮的连续流制备方法
CN114891019B (zh) * 2022-02-25 2024-06-04 复旦大学 一种乙烯基硫醚化合物的连续流制备方法
CN117358178A (zh) * 2023-12-08 2024-01-09 天津凯莱英医药科技发展有限公司 丙硫菌唑的连续化合成系统及方法
CN118162064B (zh) * 2024-05-15 2024-08-30 济南大学 一种美罗培南母核中间体的连续化生产装置及方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU201324B (en) * 1988-07-29 1990-10-28 Egyt Gyogyszervegyeszeti Gyar New process for production of substituated 1,2,4-triasole (4,3-a)-piridin-2 (2h)-on
US5900485A (en) * 1996-07-29 1999-05-04 Apotex, Inc. Methods for the manufacture of neofazodone
CN101772490A (zh) * 2007-08-03 2010-07-07 方济各安吉利克化学联合股份有限公司 纯化形式的曲唑酮和盐酸曲唑酮
CN105777745A (zh) * 2016-03-29 2016-07-20 深圳市泛谷药业股份有限公司 一种盐酸曲唑酮的制备方法

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IT1066857B (it) 1965-12-15 1985-03-12 Acraf Derivati della s ipiazolo 4.3 a piridina e processi per la loro preparazione
US4252806A (en) * 1979-09-24 1981-02-24 Mead Johnson & Company Triazoloquinolones
US4254124A (en) 1979-09-24 1981-03-03 Mead Johnson & Company Antidepressant agent
AU663057B2 (en) 1990-09-28 1995-09-28 Pharmacia & Upjohn Company Anthelmintic and anticoccidal 3-carbamoyl-4-hydroxycoumarins
IT1314283B1 (it) 1999-12-16 2002-12-06 Acraf Trazodone cloridrato ed un procedimento per prepararlo.
WO2017166050A1 (zh) * 2016-03-29 2017-10-05 深圳市泛谷药业股份有限公司 一种盐酸曲唑酮的制备方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU201324B (en) * 1988-07-29 1990-10-28 Egyt Gyogyszervegyeszeti Gyar New process for production of substituated 1,2,4-triasole (4,3-a)-piridin-2 (2h)-on
US5900485A (en) * 1996-07-29 1999-05-04 Apotex, Inc. Methods for the manufacture of neofazodone
CN101772490A (zh) * 2007-08-03 2010-07-07 方济各安吉利克化学联合股份有限公司 纯化形式的曲唑酮和盐酸曲唑酮
CN105777745A (zh) * 2016-03-29 2016-07-20 深圳市泛谷药业股份有限公司 一种盐酸曲唑酮的制备方法

Non-Patent Citations (1)

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Title
Practical Use of Continuous Processing in Developing and Scaling Up Laboratory Processes;Neal G.Anderson;《Org. Proc. Res. Dev.》;20011024;第5卷(第6期);第613-621页 *

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AU2019217490A1 (en) 2020-09-17
CN111886235A (zh) 2020-11-03
ES2916406T3 (es) 2022-06-30
JP2021512888A (ja) 2021-05-20
IL276483B2 (en) 2023-09-01
CA3089552A1 (en) 2019-08-15
PT3749668T (pt) 2022-06-02
SG11202006948XA (en) 2020-08-28
MD3749668T2 (ro) 2022-08-31
DK3749668T3 (da) 2022-06-20
SMT202200277T1 (it) 2022-09-14
AU2019217490B2 (en) 2023-06-29
EP3749668A1 (en) 2020-12-16
IL276483B1 (en) 2023-05-01
GEAP202215429A (en) 2022-05-10
MX2020008241A (es) 2022-07-25
IL276483A (en) 2020-09-30
KR20200130249A (ko) 2020-11-18
SI3749668T1 (sl) 2022-09-30
MX394182B (es) 2025-03-24
EA202091834A1 (ru) 2020-10-22
CY1125298T1 (el) 2025-03-28
UA126870C2 (uk) 2023-02-15
HUE058990T2 (hu) 2022-09-28
RS63323B1 (sr) 2022-07-29
EP3749668B1 (en) 2022-04-06
PL3749668T3 (pl) 2022-07-25
KR102646651B1 (ko) 2024-03-13
US20210032243A1 (en) 2021-02-04
BR112020015885A2 (pt) 2020-12-08
LT3749668T (lt) 2022-08-10
WO2019154770A1 (en) 2019-08-15
GEP20227417B (en) 2022-09-26
HRP20220733T1 (hr) 2022-09-02
AU2019217490A2 (en) 2020-09-24
US12221438B2 (en) 2025-02-11
JP7301858B2 (ja) 2023-07-03

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