Process for preparing prostaglandines

专利摘要:
1456511 Prostaglandins PFIZER Inc 1 Nov 1973 [8 Nov 1972] 50889/73 Heading C2C The invention comprises prostaglandins of the formula I and the C 15 epimers thereof, wherein A is Ar(CH 2 ) n - or -(CH 2 ) m -OR<SP>2</SP>, W is a single bond or cis double bond, Z is a single bond or trans double bond; m is oxo or n is 0 to 5 when Z is a single bond, or n is 1 to 5 when Z is a trans double bond; m is 2 or 3; R<SP>2</SP> is C 1-4 alkyl; Ar is α- or #-furyl, α- or #-thienyl, α- or #-naphthyl, 3,4-dimethoxyphenyl, 3,4-methylenedioxyphenyl, 3,4,5-trimethoxyphenyl or phenyl optionally monosubstituted by halogen, trifluoromethyl, phenyl, C 1-4 alkyl or C 1-4 alkoxy; R 1 is p-biphenylyl, R is H or C 1-4 alkyl, X and Y together form a single bond or X is H and Y is alpha-hydroxy, with the proviso that when X and Y form a single bond m is oxo; and compounds of the Formulµ II, III and VI or and their C 15 epimers, wherein m is oxo or Compounds of Formula I above are obtained by esterifying the corresponding acids of Formula I in which R<SP>1</SP> and X are hydrogen and Y is alpha-hydroxy with p-phenylphenol, and if desired, dehydrating the resulting compounds in which m is oxo and Y is alpha-hydroxy. The esters of the prostaglandin E and F series may also be obtained by hydrolysing the corresponding 11,15-bis-(tetrahydropyranyl) ethers of Formula VI above which are obtained by reacting compounds of the Formula VII with compounds of the formula and if desired, oxidizing and/or hydrogenating the resulting compounds of formula VI above in which m is Compounds of Formula II and III above are obtained by reacting compounds of formula VII above with compounds of the formula and if desired, oxidizing and/or hydrogenating the resulting compounds of Formula II above. Biphenylyl 9,15 - dioxo - 11α - hydroxy - 17- phenyl - 18,19,20 - trinor - cis - 5, trans - 13- prostadienoate is obtained by oxidizing biphenylyl 9 - oxo - 11α,15# - dihydroxy - 17- phenyl - 18,19,20 - trinor - cis - 5, trans - 13- prostadienoate with manganese dioxide. Pharmaceutical compositions, suitable for oral, intravaginal, intraamniotically, intravenous or intranasal administration, contain the above esters of Formula I together with suitable carriers or diluents. The compound possess similar pharmacological properties to those of the naturally occurring prostaglandins. Reference has been directed by the Comptroller to Specifications 1,386,146, 1,345,934 and 1,324,737.
公开号:SU1021340A3
申请号:SU752115232
申请日:1975-03-20
公开日:1983-05-30
发明作者:Росс Джонсон Майкл；Кен Шааф Томас；Сингх Биндра Джесит
申请人:Пфайзер Инк (Фирма)；
IPC主号:

专利说明:

tc
with
i 1,

权利要求:
Claims (1)
[1]
METHOD FOR PRODUCING PROSTAGLANDINS of the general formula.
(where M and I have the indicated meanings, they are reacted with 4-oxidaphenyl in the presence of dicyclohexylcarbo ^ diimide, followed by isolation of the target product.
- · * Λ ¢.
iiuS.iίιi Ϊ Oh
SC ST ST efl.-i
Τΐί „t-4 ΤΤΤΤΤ LC Tt _{YaET tG} NDP gave-S

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引用文献:

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公开号 | 申请日 | 公开日 | 申请人 | 专利标题

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FR2361381B1|1972-07-13|1980-04-25|Pfizer|

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US3929862A|1974-01-08|1975-12-30|Upjohn Co|Substituted tolylesters of PGF{HD 2{B {60|

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US3998869A|1974-11-14|1976-12-21|The Upjohn Company|Substituted anilide esters of 16-substituted PGE2|

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DE2737807A1|1976-08-27|1978-03-09|Pfizer|C LOW 1 -P-BIPHENYLESTER OF OMEGA-PENTANORPROSTAGLANDINES|

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US6531504B2|2001-05-17|2003-03-11|Allergan, Inc.|Prostanoic acid derivatives as agents for lowering intraocular pressure|

法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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US30481572A| true| 1972-11-08|1972-11-08|

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