BR9808486A - Processo para a preparação de um composto - Google Patents

Processo para a preparação de um composto

Info

Publication number
BR9808486A
BR9808486A BR9808486-0A BR9808486A BR9808486A BR 9808486 A BR9808486 A BR 9808486A BR 9808486 A BR9808486 A BR 9808486A BR 9808486 A BR9808486 A BR 9808486A
Authority
BR
Brazil
Prior art keywords
compound
formula
preparation
present
toluene
Prior art date
Application number
BR9808486-0A
Other languages
English (en)
Inventor
Michael E Pierce
Cheng Y Chen
Anusuya Choudhury
Lilian A Radesca
Lushi Tan
Dalian Zhao
Original Assignee
Du Pont Pharm Co
Merck & Co 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 Du Pont Pharm Co, Merck & Co Inc filed Critical Du Pont Pharm Co
Publication of BR9808486A publication Critical patent/BR9808486A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C221/00—Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

"PROCESSO PARA A PREPARAçãO DE UM COMPOSTO" A presente invenção fornece métodos para a síntese assimétrica de (S)-6-cloro-4-ciclopropiletinil-4-trifluorometil-1,4-dihidro-2H-3,1-benzo xazin-2-ona da fórmula (VI-i), que é útil como inibidor da transcriptase reversa do vírus da imunodeficiência humana (HIV). Em uma das realizações, a presente invenção fornece um processo para a preparação de um composto aminoálcool da fórmula (V-i) compreendendo a adição de uma solução em tolueno de 2,3-dicloro-5,6-diciano-1,4-benzoquinona a uma solução em tolueno de um composto da fórmula (III-i), através de um composto da fórmula (IV-i).
BR9808486-0A 1997-04-07 1998-04-02 Processo para a preparação de um composto BR9808486A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US4280397P 1997-04-07 1997-04-07
PCT/US1998/006462 WO1998045278A1 (en) 1997-04-07 1998-04-02 Asymmetric synthesis of benzoxazinones via new intermediates

Publications (1)

Publication Number Publication Date
BR9808486A true BR9808486A (pt) 2000-05-23

Family

ID=21923837

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9808486-0A BR9808486A (pt) 1997-04-07 1998-04-02 Processo para a preparação de um composto

Country Status (19)

Country Link
US (2) US5925789A (pt)
EP (1) EP0973755A1 (pt)
JP (1) JP2001519810A (pt)
KR (1) KR20010006074A (pt)
CN (2) CN1251582A (pt)
AR (1) AR014342A1 (pt)
AU (1) AU6876898A (pt)
BR (1) BR9808486A (pt)
CA (1) CA2285000A1 (pt)
EA (1) EA199900911A1 (pt)
EE (1) EE9900446A (pt)
HR (1) HRP980192A2 (pt)
HU (1) HUP0001407A3 (pt)
IL (1) IL132185A0 (pt)
NO (1) NO994836D0 (pt)
NZ (1) NZ500727A (pt)
SK (1) SK136199A3 (pt)
WO (1) WO1998045278A1 (pt)
ZA (1) ZA982956B (pt)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5965729A (en) 1997-02-05 1999-10-12 Merck & Co., Inc. Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
HU229087B1 (en) * 1997-02-05 2013-07-29 Merck Sharp & Dohme Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent
US6673372B1 (en) 1998-06-11 2004-01-06 Bristol-Myers Squibb Pharma Company Crystalline Efavirenz
TWI326283B (en) * 2002-07-31 2010-06-21 Du Pont Method for preparing fused oxazinones
EP2197273B1 (en) * 2007-10-01 2014-09-24 Ascenta Therapeutics, Inc. Process for preparing r-gossypol l-phenylalaninol dienamine
WO2009133538A1 (en) * 2008-05-01 2009-11-05 Ranbaxy Laboratories Limited Process for the preparation of efavirenz
US8420808B2 (en) 2009-01-30 2013-04-16 F.I.S. Fabbrica Italiana Sintetici S.P.A. Process for the preparation of efavirenz
US8080655B2 (en) * 2009-07-20 2011-12-20 Apotex Pharmachem Inc. Methods of making efavirenz and intermediates thereof
CN102584801B (zh) * 2011-01-06 2015-02-18 中国科学院上海有机化学研究所 Hiv逆转录酶抑制剂依法韦伦类化合物的一锅法不对称合成工艺
CN102617367A (zh) * 2012-03-08 2012-08-01 浙江江北药业有限公司 (S)-5-氯-α-（环丙基乙炔）-2-氨基-α-（三氟甲基）苯甲醇晶型的制备
CN103833560B (zh) * 2013-03-25 2016-05-25 安徽贝克联合制药有限公司 (S)-5-氯-α-环丙炔基-2-氨基-α-三氟甲基苯甲醇的制备方法
CN105001101B (zh) * 2015-05-28 2017-11-28 乐平市瑞盛制药有限公司 一种4‑氯‑2‑三氟乙酰基苯胺水合物盐酸盐的合成方法
CN105010124B (zh) * 2015-06-16 2017-06-16 湖南省作物研究所 可专用作绿肥的甘蓝型油菜的选育方法
CN105010129B (zh) * 2015-08-05 2017-06-23 江苏省农业科学院 早熟陆地棉新种质选育方法
CN105801442A (zh) * 2015-10-16 2016-07-27 浙江沙星医药化工有限公司 4-氯-2-(三氟乙酰基)苯胺盐酸盐水合物的制备方法
NL2018412B1 (en) * 2017-02-23 2018-09-17 Univ Nelson Mandela Metropolitan Method for the manufacture of efavirenz
CN108997150B (zh) * 2018-08-31 2021-01-12 江苏沙星化工有限公司 一种依法韦仑中间体的制备方法
CN108997152A (zh) * 2018-08-31 2018-12-14 江苏沙星化工有限公司 制备4-氯-2-（三氟乙酰基）苯胺盐酸盐的改进工艺
CN110204450B (zh) * 2019-05-24 2022-05-03 浙江江北药业有限公司 一种4-氯-2-三氟乙酰基苯胺盐酸盐水合物的合成方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5316731B2 (pt) * 1974-07-08 1978-06-03
US5665720A (en) * 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
IL106507A (en) * 1992-08-07 1997-11-20 Merck & Co Inc Pharmaceutical compositions containing benzoxazinones and some novel compounds of this type
WO1995020389A1 (en) * 1994-01-28 1995-08-03 Merck & Co., Inc. Benzoxazinones as inhibitors of hiv reverse transcriptase
US5663467A (en) * 1995-01-23 1997-09-02 Merck & Co., Inc. Synthesis of cyclopropylacetylene
US5633405A (en) * 1995-05-25 1997-05-27 Merck & Co., Inc. Asymmetric synthesis of (-)-6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxanzin-2-one

Also Published As

Publication number Publication date
NZ500727A (en) 2001-06-29
CN1327976A (zh) 2001-12-26
WO1998045278A1 (en) 1998-10-15
SK136199A3 (en) 2000-06-12
CA2285000A1 (en) 1998-10-15
NO994836L (no) 1999-10-04
EP0973755A1 (en) 2000-01-26
EE9900446A (et) 2000-04-17
AR014342A1 (es) 2001-02-28
HUP0001407A1 (hu) 2001-04-28
JP2001519810A (ja) 2001-10-23
EA199900911A1 (ru) 2000-04-24
ZA982956B (en) 1999-10-07
US6040480A (en) 2000-03-21
IL132185A0 (en) 2001-03-19
HUP0001407A3 (en) 2001-06-28
NO994836D0 (no) 1999-10-04
US5925789A (en) 1999-07-20
AU6876898A (en) 1998-10-30
HRP980192A2 (en) 1999-02-28
CN1251582A (zh) 2000-04-26
KR20010006074A (ko) 2001-01-15

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Legal Events

Date Code Title Description
PCP Transfer pending
HKT Transfer or change (deleted)
TE Change of address
B25D Requested change of name of applicant approved
B25G Requested change of headquarter approved
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A, 6A, 7A, 8A E 9A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1889 DE 20/03/2007.