SE8501540L - TIMOLOLMELLANPRODUKTER - Google Patents

TIMOLOLMELLANPRODUKTER

Info

Publication number
SE8501540L
SE8501540L SE8501540A SE8501540A SE8501540L SE 8501540 L SE8501540 L SE 8501540L SE 8501540 A SE8501540 A SE 8501540A SE 8501540 A SE8501540 A SE 8501540A SE 8501540 L SE8501540 L SE 8501540L
Authority
SE
Sweden
Prior art keywords
timolol
acid
tartaric acid
tartaric
hydroxypropoxy
Prior art date
Application number
SE8501540A
Other languages
Swedish (sv)
Other versions
SE463101B (en
SE8501540D0 (en
Inventor
H Nupponen
L Hietaniemi
Original Assignee
Star Oy Ab
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 Star Oy Ab filed Critical Star Oy Ab
Publication of SE8501540D0 publication Critical patent/SE8501540D0/en
Publication of SE8501540L publication Critical patent/SE8501540L/en
Publication of SE463101B publication Critical patent/SE463101B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The novel dialkanoyl, diaroyl or alkanoyl-aroyl L-tartaric acid-O-monoesters of 3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiazol e correspond to the formula <IMAGE> (R = the alkyl or aryl group). They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiaz ole, i.e. of S-timolol, which has useful beta -blocking activity, as well as of its acid addition salts. The said L-tartaric acid-O-monoesters are prepared from the corresponding L-tartaric anhydride and R,S-timolol, and their resolution is carried out by crystallising the racemic ester from an alcohol or from a mixture of alcohol and water in a pH range from 7 to 2, resulting in the isolation of the L-tartaric acid-O-monoester of S-timolol in optically pure form, from which ester S-timolol is liberated by acid hydrolysis and can be converted to the desired acid salt.
SE8501540A 1984-03-30 1985-03-28 L-TIN ACID O-MONOESTERS OF 3-MORPHOLINO-4- (3'-TERT-BUTYLAMINO-2'-HYDROXYPROPOXY) -1,2,5-THIADIAZOL, PROCEDURES FOR PREPARING THEREOF AND THEIR USE AS A PREPARATION OF INTERMEDIATE PREPARATION 3-morpholino-4- (3-tertbutylamino-2'HYDROXIPROPOXI) -1,2,5-thiadiazol SE463101B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FI841292A FI71933C (en) 1984-03-30 1984-03-30 New L-tartaric acid O-monoesters of 3-morpholino-4- (3'-tert.-butylamino-2'-hydroxypropoxy) -1,2,5-thiadiazole and their use as intermediates.

Publications (3)

Publication Number Publication Date
SE8501540D0 SE8501540D0 (en) 1985-03-28
SE8501540L true SE8501540L (en) 1985-10-01
SE463101B SE463101B (en) 1990-10-08

Family

ID=8518831

Family Applications (1)

Application Number Title Priority Date Filing Date
SE8501540A SE463101B (en) 1984-03-30 1985-03-28 L-TIN ACID O-MONOESTERS OF 3-MORPHOLINO-4- (3'-TERT-BUTYLAMINO-2'-HYDROXYPROPOXY) -1,2,5-THIADIAZOL, PROCEDURES FOR PREPARING THEREOF AND THEIR USE AS A PREPARATION OF INTERMEDIATE PREPARATION 3-morpholino-4- (3-tertbutylamino-2'HYDROXIPROPOXI) -1,2,5-thiadiazol

Country Status (9)

Country Link
AT (1) AT391696B (en)
CH (1) CH663208A5 (en)
DD (1) DD234011A5 (en)
DK (1) DK162283C (en)
FI (1) FI71933C (en)
NL (1) NL192386C (en)
NO (1) NO158020C (en)
SE (1) SE463101B (en)
SU (1) SU1417798A3 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988007044A1 (en) * 1987-03-17 1988-09-22 Insite Vision, Inc. Timolol derivatives
FI82240C (en) * 1988-10-20 1991-02-11 Huhtamaeki Oy FOERFARANDE FOER FRAMSTAELLNING AV PHARMACOLOGISKT VAERDEFULLT S-TIMOLOL-HEMIHYDRAT.

Also Published As

Publication number Publication date
SE463101B (en) 1990-10-08
NL8500939A (en) 1985-10-16
SU1417798A3 (en) 1988-08-15
DK162283B (en) 1991-10-07
CH663208A5 (en) 1987-11-30
FI71933B (en) 1986-11-28
FI841292A (en) 1985-10-01
FI841292A0 (en) 1984-03-30
ATA87685A (en) 1990-05-15
SE8501540D0 (en) 1985-03-28
DK162283C (en) 1992-03-02
NL192386C (en) 1997-07-04
NL192386B (en) 1997-03-03
DK142885D0 (en) 1985-03-29
NO851307L (en) 1985-10-01
AT391696B (en) 1990-11-12
DD234011A5 (en) 1986-03-19
NO158020C (en) 1990-05-02
DK142885A (en) 1985-10-01
FI71933C (en) 1989-04-06
NO158020B (en) 1988-03-21

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