FI108434B - F÷rfarande f÷r framstõllning av farmakologiskt verksamma bensimidazolderivat - Google Patents

F÷rfarande f÷r framstõllning av farmakologiskt verksamma bensimidazolderivat Download PDF

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FI108434B
FI108434B FI911936A FI911936A FI108434B FI 108434 B FI108434 B FI 108434B FI 911936 A FI911936 A FI 911936A FI 911936 A FI911936 A FI 911936A FI 108434 B FI108434 B FI 108434B
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methyl
compound
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biphenyl
benzimidazole
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Kohei Nishikawa
Takehiko Naka
Takeshi Kato
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Takeda Chemical Industries Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/28—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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Claims (4)

1. Ett förfarande för framställning av en terapeutiskt aktiv förening med formeln (I) ΓΊ' · N^/NH där Y är -O-, -S- eller -N(H)-; och D' är hydroxi, Ci_g-alkoxi, som valbart kan vara substituerad med 5-metyl-2-oxi-l,3-dioxolen-4-yl, C2-3-alkenyloxi, som valbart kan vara substituerad med fenyl, eller en grupp, vars formel är -OCH(R7)OCOR8, där R7 är väte eller C^.g-alkyl och R8 är Ci_g-alkylf C5_7-cykloalkyl, fenyl, C^.g-alkoxi eller C5_7-cykloalkoxi, eller ett farmaceutiskt acceptabelt sait därav, kännetecknatav att (i) en förening med formeln (II) D'-OC H (II) @5“ 'alkyl • · där Y och D' betyder samma som definierats ovan, bringas att reagera med en förening med formeln (III) 'nJH (III) Z-CH 2^\0)~~\0/ där Z är halogen; ♦ 104 108414 (ii) en förening med formeln (IV) d'-oc Oy-~-^Oy dv) [pYNH rv S^KH2 n^n där D1 betyder samma som definierats ovan, bringas att reagera med alkylortokarbonat, en karbonylerande eller tiokarbonyle-rande reagens eller isotiocyanat, (iii) en förening med formeln (V) N=T (V) D’-OC CH2-(g>—(Ö) där alla grupper betyder samma som definierats ovan, bringas att reagera med en nukleofil reagens, (iv) en förening med formeln (Ia) * i · • « CU D' -0CL -\°) (Ia) * där alla grupper betyder samma som definierats ovan, bringas att reagera med en azid; t · «(. 108434 105 (v) en förening tried formeln (Ij) Π ΝγΝΗ R500C -(5) (Ij) CsX^-^i-e -alkyl där R5 är Ci_g-alkyl och Y betyder sarama som definierats ovan, bringas i hydrolys, varvid erhälls en förening med formeln (Ik) ΓΊ ΝγΝΗ “I (f) -alkyl där Y betyder sarama som definierats ovan; eller (vi) en förening med formeln (II) • I N-*l_ / D’-oc -alkyl ^ · där R är en skyddande grupp och de övriga grupperna betyder sarama som definierats ovan, bringas i en skyddsgruppselimine-rande reaktion, och om sä önskas den förening som erhallits med reaktionerna (i)-(vi) omvandlas * ‘ tili en förening med formeln (I) genom hydrolys, nukleofil 106 1 0 8 4 3 4 reaktion, esterifiering och/eller genom att eliminera skydds-gruppen i tetrazolringen pä vanligt sätt, säsom genom en reaktion med syra, ooh om sä önskas föreningen med formeln (I) omvandlas till dess farmaceutiskt acceptabla sait, ooh eventuellt, att slutprodukten kristalliseras frän ett lösnings-medel, sora valts ur en grupp bestäende av lägre alkoholer, blandningar av lägre alkoholer och vatten och blandningar av lägre alkylketoner och vatten.
2. Förfarande enligt patentkravet 1, kännetecknat av att man framställer en förening med formeln (I) , som är 2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimi-dazol-7- karboxylsyra, eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I) som är 2-prop-oxi-1-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I) som är metyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimid-azol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller V ’ att man framställer en förening med formeln (I) som är pivalo-yloximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I) som är 2-met-.. · , oxi-1-[ [2 ' - (lH-tetrazol-5-yl) bifenyl-4-yl] metyl] bensimidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I) som är (5-me-tyl-2-oxo-l,3-dioxolen-4-yl)metyl-2-etoxi-l-[[21 -(lH-tetrazol- * i 107 ^ 08 434 5-yl)bifenyl-4-yl]metyl]bensimidazol-7^karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) som är 1-(cyk- lo-hexyloxikarbonyloxi)etyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt.
3. Förfarande enligt patentkravet 1, kännetecknat av att man framställer en förening med formeln (I) , som är etyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är etyl-2-propoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är etyl-2-metyltio-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl] metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är etyl-2-etyltio-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är etyl-> *·' 2-propyltio-1- [ [2 1 - (ΙΗ-tetrazol-5-yl) bif enyl-4 -yl] metyl] bens- imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställler en förening med formeln (I), som är 2-me-tyltio-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens- • · « v ice 108434 imidazoi-7-karboxylsyra eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är 2-etyl-tio-1-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är 2-propyltio-1-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är etyl-2-etylamino-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är etyl-2-propylamino-1-[[21 -(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är metyl-2-metoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är 2-etyl-amino-1-[[2'- (1H-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är 2 - 1 propylamino-1-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bens-imidazol-7-karboxylsyra eller dess farmaceutiskt acceptabla salt, eller V · · «. 109 108434 att man f rams taller en förening med formeln (I) , som är acet-oximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]-bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller t att man framställer en förening med formeln (I), som är propio-nyloximetyl-2-etoxi-l-[ [2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är buty-ryloximetyl-2-etoxi-l- [ [2'-(lH-tetrazol-5-yl)bifenyl-4-yl] -metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I) , som är iso-butyryloximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller att man framställer en förening med formeln (I), som är 1-(et-oxikarbonyloxi)etyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl- 4-yl] metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller • · r • · att man framställer en förening med formeln (I), som är 1-acet-oxietyl-2-etoxi-l-[[21 -(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]-bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller t V att man framställer en förening med formeln (I) , som är 1- (iso-propoxikarbonyloxi)etyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla salt, eller • · o <. . 110 1 08434 att man framställer en förening med formeln (I), som är cyklo-hexylkarbonyloximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl- 4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I) , som är bensoyloximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I), som är (E)-cinnamoyloximetyl-2-etoxi-l-[[21 -(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I), som är cyklo-pentylkarbonyloximetyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bi-fenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, e],.ler att man framställer en förening med formeln (I), som är pivalo-yloximetyl-2-etylamino-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]-metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait, eller att man framställer en förening med formeln (I), som är 1-(cyk-lohexyloxikarbonyloxi)etyl-2-etylamino-l-[[21 -(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait.
: · - 4. Förfarande enligt patentkravet 1, kännetecknat av att man framställer en förening med formeln (I), som är 1-(cyklohexyloxikarbonyloxi)etyl-2-etoxi-l-[[2'-(lH-tetrazol-5-yl)bifenyl-4-yl]metyl]bensimidazol-7-karboxylat eller dess farmaceutiskt acceptabla sait. * · <
FI911936A 1990-04-27 1991-04-22 F÷rfarande f÷r framstõllning av farmakologiskt verksamma bensimidazolderivat FI108434B (sv)

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US5196444A (en) * 1990-04-27 1993-03-23 Takeda Chemical Industries, Ltd. 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and compositions and methods of pharmaceutical use thereof
DE4036706A1 (de) * 1990-11-17 1992-05-21 Hoechst Ag Verfahren zur behandlung der cardialen sowie der vasculaeren hypertrophie und hyperplasie
GB9027208D0 (en) * 1990-12-14 1991-02-06 Smithkline Beecham Plc Medicaments
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