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公开(公告)号:US3290226A
公开(公告)日:1966-12-06
申请号:US34587064
申请日:1964-02-19
申请人: UPJOHN CO
发明人: BEAL III PHILIP F , FONKEN GUNTHER S , PIKE JOHN E
IPC分类号: C07C405/00 , C12P31/00
CPC分类号: C07C405/00 , C12P31/00 , Y10S435/866 , Y10S435/872 , Y10S435/874 , Y10S435/886 , Y10S435/912 , Y10S435/913 , Y10S435/933 , Y10S435/939
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12.
公开(公告)号:US09346738B2
公开(公告)日:2016-05-24
申请号:US14401826
申请日:2013-05-22
申请人: SciPharm SàRL
IPC分类号: C07C59/115 , C07C51/377 , C07C47/565 , C07C47/575 , C07F7/18 , C07C59/72 , C12P31/00 , C12P41/00
CPC分类号: C07C51/377 , C07C47/565 , C07C47/575 , C07C59/72 , C07C2603/14 , C07F7/18 , C07F7/1804 , C07F7/1892 , C12P31/00 , C12P41/002 , C12P41/004
摘要: A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.
摘要翻译: 描述了曲前列素及其衍生物的制备方法。 与现有技术相反,该方法利用关键中间体易于扩展的酶分解来制备这些化合物。 所述方法与现有方法的另一重大改进是5-烯丙氧基 - 苯甲醛前体的区域选择性Claisen重排,其由2-位的溴取代基促进。
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公开(公告)号:US20060247453A1
公开(公告)日:2006-11-02
申请号:US11369518
申请日:2006-03-06
IPC分类号: C07C401/00
CPC分类号: C12P31/00 , C12P41/004
摘要: A method for the selective enzymatic acetylation of a bimatoprost intermediate is provided.
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公开(公告)号:US4190670A
公开(公告)日:1980-02-26
申请号:US831949
申请日:1977-09-09
申请人: Arthur F. Marx , Jean Doodewaard
发明人: Arthur F. Marx , Jean Doodewaard
IPC分类号: C07C405/00 , C07F1/00 , C07F1/08 , C12P31/00 , C07C177/00
CPC分类号: C12P31/00 , C07C405/00 , C07F1/00 , C07F1/08
摘要: Novel 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives of the formula I ##STR1## wherein the dotted line in the position 8-12 indicates the optional presence of a double bond, the waved lines in position 15 indicate that the hydroxyl group and the group R.sub.4 are either in .alpha.- or .beta.-position and Z represents a --CH.sub.2 CH.sub.2 -- or a cis --CH.dbd.CH-- group, and wherein R represents one of the groups: ##STR2## (wherein the waved lines indicate that the hydroxyl groups are either in .alpha.- or .beta.-position and R.sub.1 represents a hydrogen atom, a methyl or ethyl group), R.sub.2 represents either an oxygen atom or a hydrogen atom and an .alpha.- or .beta.-hydroxyl group, R.sub.3 represents a hydrogen atom or a hydroxyl group and R.sub.4 represents a hydrogen atom or a methyl group, with the proviso that when simultaneously, R.sub.1, R.sub.3 and R.sub.4 each represents a hydrogen atom, R.sub.2 represents an oxygen atom, a double bond is in 8-12 position and the 15-hydroxyl group is in position .alpha., R does not represent the group (b), but that when in addition to these conditions, Z represents a cis --CH.dbd.CH-- group and the 8-12 position is saturated, R either represents the groups (b) or (c); and the pharmaceutically acceptable salts and esters thereof, novel process for their preparation by selective microbiological hydroxylation of compounds formula II ##STR3## wherein the dotted line in the position 10-11 indicates the optional presence of a double bond in case the 8-12 position is saturated and the other symbols are as defined hereinabove, by means of microorganisms of the Division of Eumycota or, as far as the introduction of a hydroxyl group in the 18- or 19-position is concerned, of the Family of Streptomycetaceae, and, if desired, conversion of the 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives thus obtained into pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions containing at least one of the novel hydroxy-prostaglandin derivatives of formula I.
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公开(公告)号:US3983153A
公开(公告)日:1976-09-28
申请号:US530430
申请日:1974-12-06
申请人: William P. Schneider
发明人: William P. Schneider
IPC分类号: C07C35/27 , C07C405/00 , C07D309/12 , C07D317/26 , C07D317/30 , C12P31/00 , C07C177/00
CPC分类号: C07D309/12 , C07C35/27 , C07C405/00 , C07D317/26 , C07D317/30 , C12P31/00
摘要: This invention is racemic PGE.sub.2, racemic PGF.sub.2 .sub..alpha., racemic PGF.sub.2 .sub..beta., racemic PGA.sub.2, racemic PGB.sub.2, analogs of those, and processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, abortion, and wound healing.
摘要翻译: 本发明是外消旋PGE2,外消旋PGF2α,外消旋PGF2β,外消旋PGA2,外消旋PGB2,其类似物及其制备方法。 这些化合物可用于各种药理学目的,包括抗溃疡,抑制血小板聚集,增加鼻通气,流产和伤口愈合。
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公开(公告)号:US3974200A
公开(公告)日:1976-08-10
申请号:US530434
申请日:1974-12-06
申请人: William P. Schneider
发明人: William P. Schneider
IPC分类号: C07C35/27 , C07C405/00 , C07D309/12 , C07D317/26 , C07D317/30 , C12P31/00 , C07C177/00
CPC分类号: C12P31/00 , C07C35/27 , C07C405/00 , C07D309/12 , C07D317/26 , C07D317/30
摘要: This invention is racemic PGE.sub.2, racemic PGF.sub.2.sub..alpha., racemic PGF.sub.2.sub..beta. , racemic PGA.sub.2, racemic PGB.sub.2, analogs of those, and processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, abortion, and wound healing.
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17.
公开(公告)号:US3970685A
公开(公告)日:1976-07-20
申请号:US476362
申请日:1974-06-05
申请人: Karl G. Untch , Gilbert J. Stork
发明人: Karl G. Untch , Gilbert J. Stork
IPC分类号: A61K31/10 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C12P31/00 , C07C147/14
CPC分类号: C07C405/00 , C07C405/0033 , C07D309/12 , C12P31/00
摘要: (dl)-13-Substituted sulfinyl-prostaglandin-like [(dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (dl)-2.alpha.-substituted -3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-4-oxygenated-1-oxygenated cyclopentane] compounds exhibit prostaglandin-like biological properties and are also useful intermediates in the preparation of known prostaglandins.
摘要翻译: (dl)-13-取代的亚磺酰基 - 前列腺素样[(dl)-2α-取代-3β-(1α-取代的亚磺酰基 - 反式-2-烯基)-1-氧化环戊烷和(dl)-2α 取代-3β-(1α-取代亚磺酰基 - 反式-2-烯基)-4-氧化-1-氧化环戊烷]化合物表现出前列腺素样生物学性质,并且也是制备已知前列腺素的有用的中间体。
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公开(公告)号:US3875003A
公开(公告)日:1975-04-01
申请号:US28809172
申请日:1972-09-11
发明人: STADLER ISTVAN , KOVACS GABOR , MESZAROS ZOLTAN , RADOCZI JULIA , SIMONIDESZ VILMOS , SZANTAY CSABA , SZEKELY ISTVAN , SZATHMARY CSABA
IPC分类号: C07C405/00 , C12P31/00 , C12D1/02
CPC分类号: C12P31/00 , C07C405/00
摘要: A process for producing a prostaglandin, comprising decomposing an ester selected from the group which consists of:
-(CHz)6-COOR1 or -CH2-(CH CH)-(CH2)3-COOR1 in Alpha or Beta steric position and R1 is alkyl having 1 to 4 carbon atoms, at a pH between 6 and 8.5 with an ester hydrolase enzyme (EC.3.1.1) selected from the group which consists of lipase, carboxylesterhydrolase, cholesterolesterase, acetyl-cholinesterase and acetylesterase.-
公开(公告)号:US3852337A
公开(公告)日:1974-12-03
申请号:US28295272
申请日:1972-08-23
发明人: BERGSTROM S , SJOVALL J
CPC分类号: C12P31/00 , B01J23/42 , C07C405/00 , C07C405/0016 , Y10S514/935
摘要: There are disclosed compounds of the formula:
WHEREIN Y is -CH2CH2- or trans-CH CH-, and both X and Z are CH2CH2-, or wherein Y is trans-CH CH-, X is cis-CH CH-, and Z is -CH2CH2- or cis-CH CH-, wherein R is hydrogen or lower alkanoyl, and wherein * indicates attachment of -OR to the ring in alpha or beta configuration. These novel compounds are useful for a variety of pharmacological purposes, including use as smooth muscle stimulants.摘要翻译: 公开了下式的化合物:
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公开(公告)号:US3839409A
公开(公告)日:1974-10-01
申请号:US36767873
申请日:1973-06-06
发明人: BERGSTROM S , SJOVALL J
CPC分类号: C07C405/00 , B01J23/42 , C07C405/0016 , C12P31/00
摘要: 1. A COMPOUND OF THE FORMULA:
1-(O=),2-(R3-OOC-(CH2)3-CH=CH-CH2-),3-(CH3-(CH2)4-
CH(-O-R2)-CH=CH-),4-(R2-O-)CYCLOPENTANE
WHEREIN R3 IS HYDROCARBYL OF ONE TO 13 CARBON ATOMS, INCLUSIVE, AND R2 IS HYDROGEN OR LOWER ALKANOYL.
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