YU48951B - ENANTIOSELEKTIVNA SINTEZA JEDINJENJA TIENO (2,3-b)-TIOPIRAN-7,7-DIOKSIDA - Google Patents

ENANTIOSELEKTIVNA SINTEZA JEDINJENJA TIENO (2,3-b)-TIOPIRAN-7,7-DIOKSIDA

Info

Publication number
YU48951B
YU48951B YU13194A YU13194A YU48951B YU 48951 B YU48951 B YU 48951B YU 13194 A YU13194 A YU 13194A YU 13194 A YU13194 A YU 13194A YU 48951 B YU48951 B YU 48951B
Authority
YU
Yugoslavia
Prior art keywords
thiopyran
thieno
enantioselective synthesis
dioxide compounds
dioxide
Prior art date
Application number
YU13194A
Other languages
English (en)
Other versions
YU13194A (sh
Inventor
Sohar Paul
J. Mathire David
J. Blacklock Thomas
Original Assignee
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 Merck & Co.Inc. filed Critical Merck & Co.Inc.
Publication of YU13194A publication Critical patent/YU13194A/sh
Publication of YU48951B publication Critical patent/YU48951B/sh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Seasonings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Postupak za dobijanje jedinjenja strukturne formule I: i njegove hidrohloridne soli, gde je hiralnost na C-6 fiksna, i zadržan je trans-stereohemijski odnos između C-4 i C-6 supstituenata, jedinjenje je kristalno, a R i R1 su isti ili različiti i oni su C1-3 alkil, naznačen time, što obuhvata stupnjeve: A tretiranje jedinjenja formule II sa nitrilom formule RCN i jakom kiselinom, tako da je količina vode koja je prisutna, u zavisnosti od upotrebljene kiseline, od oko 0,5 do oko 10 tež%, pri čemu se dobija jedinjenje strukture III: B) tretiranje III sa hlorsulfo kiselinom, pri čemu se dobija jedinjenje strukture IV: C) tretiranje IV sa tionil hloridom, pri čemu se dobija jedinjenje strukture V: D) tretiranje V sa amonijakom, pri čemu se dobija jedinjenje strukture VI: E) tretiranje VI sa natrijum borhidridom i jakom kiselinom, ili boran-tetrahidrofuranom, pri čemu se dobija jedinjenje strukture VII: F) izolovanje VII kao maleatne soli VIII; G) konverzija VIII u hidrohloridnu so jedinjenja I; i H) prečišćavanje hidrohloridne soli jedinjenja I. Prijava sadrži još 7 zavisnih zahteva.
YU13194A 1993-03-22 1994-03-21 ENANTIOSELEKTIVNA SINTEZA JEDINJENJA TIENO (2,3-b)-TIOPIRAN-7,7-DIOKSIDA YU48951B (sh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3552393A 1993-03-22 1993-03-22
US19588694A 1994-02-10 1994-02-10

Publications (2)

Publication Number Publication Date
YU13194A YU13194A (sh) 1997-01-08
YU48951B true YU48951B (sh) 2003-01-31

Family

ID=26712200

Family Applications (1)

Application Number Title Priority Date Filing Date
YU13194A YU48951B (sh) 1993-03-22 1994-03-21 ENANTIOSELEKTIVNA SINTEZA JEDINJENJA TIENO (2,3-b)-TIOPIRAN-7,7-DIOKSIDA

Country Status (29)

Country Link
US (1) US5688968A (sh)
EP (1) EP0617037B1 (sh)
JP (1) JP3273096B2 (sh)
KR (1) KR0157162B1 (sh)
CN (1) CN1046732C (sh)
AT (1) ATE163291T1 (sh)
AU (1) AU673409B2 (sh)
BR (1) BR9406017A (sh)
CA (1) CA2119218C (sh)
CY (1) CY2108B1 (sh)
CZ (1) CZ281390B6 (sh)
DE (1) DE69408550T2 (sh)
DK (1) DK0617037T3 (sh)
ES (1) ES2112482T3 (sh)
FI (1) FI107384B (sh)
GR (1) GR3026178T3 (sh)
HK (1) HK1009063A1 (sh)
HR (1) HRP940182B1 (sh)
HU (1) HU217363B (sh)
NO (1) NO313240B1 (sh)
NZ (1) NZ263092A (sh)
PL (1) PL176373B1 (sh)
RO (1) RO115264B1 (sh)
SI (1) SI9420016B (sh)
SK (1) SK280831B6 (sh)
TW (1) TW265343B (sh)
UA (1) UA41921C2 (sh)
WO (1) WO1994021645A1 (sh)
YU (1) YU48951B (sh)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5760249A (en) * 1995-08-29 1998-06-02 Merck & Co., Inc. Synthesis of hydroxysulfone and related compounds
ES2177415B1 (es) * 2000-09-04 2004-10-16 Ragactives, S.L. Procedimiento para la obtencion de 4-alquilamino-5, 6-dihidro-4h-tieno-(2,3b)-tiopiran-2-sulfonamida-7-dioxidos, e intermedios.
ES2204306B1 (es) * 2002-08-16 2005-08-01 Ragactives, S.L. Formas polimorficas de clorhidrato de dorzolamida, su obtencion y composiciones farmaceuticas que las contienen.
EP1611138A1 (en) * 2003-04-07 2006-01-04 Hetero Drugs Limited A novel crystalline form of dorzolamide hydrochloride
WO2006038222A1 (en) * 2004-07-09 2006-04-13 Fdc Ltd AN IMPROVED PROCESS FOR THE PREPARATION OF 5,6 -DIHYDRO -4H-4(S)-ETHYLAMINO-6(S)-METHYLTHIENO[2,3-b] THIOPYRAN-2-SULFONAMIDE- 7,7 -DIOXIDE AND ITS SALT
ES2253112B1 (es) * 2004-11-05 2007-03-16 Ragactives, S.L. Procedimiento para la obtencion de derivados de 4-(n-alquilamino)-5, 6-dihidro-4h-tieno-(2,3-b)-tiopirano.
WO2006070387A1 (en) * 2004-12-28 2006-07-06 Council Of Scientific And Industrial Research PROCESS FOR PREPARING 5,6-DIHYDRO-4-(S)-(ETHYLAMINO)-6-(S) METHYL-4H-THIENO[2,3b]THIOPYRAN-2-SULPHONAMIDE-7,7-DIOXIDE HCI
US7109353B2 (en) 2004-12-28 2006-09-19 Council Of Scientific And Industrial Research Process for preparing 5,6-dihydro-4-(S)-(ethylamino)-6-(S) methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide HCl
WO2006074230A2 (en) * 2005-01-06 2006-07-13 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Method of making dorzolamide hydrochloride
JP2008526780A (ja) * 2005-01-18 2008-07-24 テバ ジョジセルジャール ザ−トケルエン ムケド レ−スベニュタ−ルシャシャ−グ ドルゾルアミド塩酸塩の非晶質および結晶質の形態およびそれらを製造する方法
JP2010526127A (ja) 2007-05-07 2010-07-29 シプラ・リミテッド ドルゾラミドの製造方法
US8927740B2 (en) 2011-03-10 2015-01-06 Zach System S.P.A. Asymmetric reduction process
ITMI20121165A1 (it) * 2012-07-03 2014-01-04 Zach System Spa Processo di riduzione asimmetrica
MX2016004940A (es) * 2013-10-17 2016-06-28 Dow Agrosciences Llc Proceso para la preparacion de compuestos plaguicidas.
US9102655B2 (en) * 2013-10-17 2015-08-11 Dow Agrosciences Llc Processes for the preparation of pesticidal compounds
CN103497202B (zh) * 2013-10-23 2015-12-02 武汉武药科技有限公司 盐酸多佐胺中间体的合成方法
CN108822127B (zh) * 2018-05-30 2020-05-15 沈阳药科大学 4-羟亚胺基噻吩并[2,3-b]噻喃-2-甲酰胺类化合物及其用途

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4863922A (en) * 1984-12-12 1989-09-05 Merck & Co., Inc. Substituted aromatic sulfonamides as antiglaucoma agents, compositions and use
US4797413A (en) * 1986-05-14 1989-01-10 Merck & Co., Inc. Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
US4968814A (en) * 1990-04-18 1990-11-06 Merck & Co., Inc. (S)-Alkyl 3-(thien-2-ylthio)butyrate and analogs and synthesis thereof
US5091409A (en) * 1990-05-17 1992-02-25 Merck & Co., Inc. 4-alkylamino-6-(C3-5 -hydrocarbyl)thieno[2,3-B]thiopyran-2-sulfonamide-7,7-dioxides

Also Published As

Publication number Publication date
HRP940182B1 (en) 2000-02-29
JP3273096B2 (ja) 2002-04-08
NO953733D0 (no) 1995-09-21
DK0617037T3 (da) 1998-03-16
PL176373B1 (pl) 1999-05-31
BR9406017A (pt) 1995-12-19
CY2108B1 (en) 2002-04-26
RO115264B1 (ro) 1999-12-30
KR0157162B1 (ko) 1998-11-16
NZ263092A (en) 1997-12-19
TW265343B (sh) 1995-12-11
ATE163291T1 (de) 1998-03-15
CA2119218C (en) 2000-02-15
EP0617037B1 (en) 1998-02-18
CA2119218A1 (en) 1994-09-23
FI954438A0 (fi) 1995-09-20
AU673409B2 (en) 1996-11-07
CN1046732C (zh) 1999-11-24
SK116995A3 (en) 1997-06-04
NO953733L (no) 1995-09-21
AU5787194A (en) 1994-09-29
HU217363B (hu) 2000-01-28
FI107384B (fi) 2001-07-31
SK280831B6 (sk) 2000-08-14
PL310633A1 (en) 1995-12-27
HK1009063A1 (en) 1999-05-21
YU13194A (sh) 1997-01-08
DE69408550T2 (de) 1998-08-27
FI954438A (fi) 1995-09-20
HRP940182A2 (en) 1996-08-31
UA41921C2 (uk) 2001-10-15
HU9502772D0 (en) 1995-11-28
SI9420016A (en) 1996-06-30
CZ281390B6 (cs) 1996-09-11
NO313240B1 (no) 2002-09-02
GR3026178T3 (en) 1998-05-29
HUT72676A (en) 1996-05-28
ES2112482T3 (es) 1998-04-01
CZ241895A3 (en) 1996-01-17
EP0617037A1 (en) 1994-09-28
US5688968A (en) 1997-11-18
JPH06298767A (ja) 1994-10-25
WO1994021645A1 (en) 1994-09-29
CN1119866A (zh) 1996-04-03
DE69408550D1 (de) 1998-03-26
SI9420016B (sl) 2002-12-31

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