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1. 发明授权

US5013864A Process for preparation of .alpha.-alkoxy acetic acids and their salts 失效
标题翻译： α-烷氧基乙酸及其盐的制备方法
公开(公告)号：US5013864A
公开(公告)日：1991-05-07
申请号：US447766
申请日：1989-12-08
申请人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
发明人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A. Partis
IPC分类号： C07C51/367 , C07C59/125 , C07C59/13 , C07C59/66 , C07C319/20 , C07C323/12 , C07C323/20
CPC分类号： C07C323/20 , C07C51/367
摘要： A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R--OH wherein R is alkyl, substituted alkyl, or cycloalkyl, or cycloalkyl alkyl with a base in an aprotic organic solvent to give an alkoxide followed by removal of the organic solvent and reaction of the alkoxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding alkoxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the alkoxy acetate salt with an acid.

2. 发明授权

US4952710A Cyclopenteneheptenoic acid derivatives and method of preparation thereof 失效
标题翻译：环戊烯庚酸衍生物及其制备方法
公开(公告)号：US4952710A
公开(公告)日：1990-08-28
申请号：US255179
申请日：1988-10-07
申请人： Kevin A. Babiak , Arthur L. Campbell
发明人： Kevin A. Babiak , Arthur L. Campbell
IPC分类号： B01J31/22 , C07B61/00 , C07C29/32 , C07C35/06 , C07C41/48 , C07C43/315 , C07C51/353 , C07C59/46 , C07C67/343 , C07C69/732 , C07D303/40 , C07D307/20 , C07D309/12 , C07D317/20 , C07D493/08 , C07F7/18 , C07F7/22
CPC分类号： C07D493/08 , C07C43/315 , C07D303/40 , C07D309/12 , C07D317/20 , C07C2101/10 , Y02P20/55
摘要： This invention relates to a novel cyclopenteneheptenoic acid derivative having the following formula ##STR1## wherein R.sub.1 is hydrogen, --COCH.sub.3, --COCF.sub.3, --CO--phenyl, or a hydroxyl protecting group such as tetrahydropyranyl, tetrahydrofuranyl, or tri-lower alkylsilyl;wherein R.sub.2 is --CH.sub.2 OR.sub.1, --COOH, --COOR, --CHO, --CH.sub.2 --OSi(R.sub.12).sub.3, ##STR2## wherein R is lower alkyl and each R.sub.12 is independently lower alkyl or aryl; andwherein Y is ethylene, cis-vinylene, trans-vinylene, or acetylene.Also disclosed is a novel process for preparation of the above-defined cyclopenteneheptenoic acid derivative. This process involves coupling of a higher order cuprate complex with a chiral cyclopentene compound. The resultant product is particularly useful as a starting compound for high yield synthesis of optically active prostaglandins.

3. 发明授权

US4812474A Kojic acid ether-ester derivatives 失效
标题翻译：曲酸醚 - 酯衍生物
公开(公告)号：US4812474A
公开(公告)日：1989-03-14
申请号：US142982
申请日：1988-01-12
申请人： Arthur L. Campbell , Masateru Miyano
发明人： Arthur L. Campbell , Masateru Miyano
IPC分类号： C07D309/40 , A61K31/35 , C07D309/32
CPC分类号： C07D309/40
摘要： Kojic acid ether-ester derivatives of formula I ##STR1## are useful pharmacological agents for the prevention, management or alleviation of elastase mediated diseases or conditions.
摘要翻译：式I的曲酸醚酯衍生物是用于预防，控制或缓解弹性蛋白酶介导的疾病或病症的有用的药理学试剂。

4. 发明授权

US4910310A Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 失效
标题翻译： N-取代的1,5-二脱氧-1,5-亚氨基-L-岩藻糖醇衍生物的合成
公开(公告)号：US4910310A
公开(公告)日：1990-03-20
申请号：US252846
申请日：1988-10-03
申请人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
发明人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
IPC分类号： C07D307/62 , C07C211/46 , C07D211/46 , C07D491/04 , C07D491/056 , C07D493/04 , C07H9/04
CPC分类号： C07D491/04 , C07D211/46
摘要： Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-.omega.-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.

5. 发明授权

US4777275A Process of preparing higher order cuprate complexes 失效
标题翻译：制备高阶铜酸盐络合物的方法
公开(公告)号：US4777275A
公开(公告)日：1988-10-11
申请号：US59695
申请日：1987-06-09
申请人： Arthur L. Campbell , James R. Behling
发明人： Arthur L. Campbell , James R. Behling
IPC分类号： C07B37/04 , C07C67/00 , C07C401/00 , C07C405/00 , C07F1/08 , C07F7/18 , C07F7/22
CPC分类号： C07F7/2212 , C07C405/00 , C07F1/08
摘要： This invention encompasses a process for preparing higher order cuprate complexes which contain a carbanion for the formation of carbon to carbon bonds in reactions such as 1,4-conjugate addition. The complex is formed by reacting a first cuprate complex with a stannane such that the carbanion to be used to form carbon to carbon bonds is transferred from the stannane to the first cuprate complex to form a different higher order cuprate complex. This process permits the in situ preparation of a higher order cuprate complex having the carbanion desired to be used in a synthetic reaction. Higher order cuprate complexes prepared by this process are particularly useful for the efficient preparation of pharmacologically active prostaglandins.

6. 发明授权

US6127556A Epoxide formation by continuous in-situ synthesis process 失效
标题翻译：通过连续原位合成过程形成环氧化物
公开(公告)号：US6127556A
公开(公告)日：2000-10-03
申请号：US991598
申请日：1997-12-16
申请人： Chin Liu , John S. Ng , James R. Behling , Arthur L. Campbell
发明人： Chin Liu , John S. Ng , James R. Behling , Arthur L. Campbell
IPC分类号： C07D301/00 , C07C213/04 , C07C215/28 , C07D301/02 , C07D301/30 , C07D303/36 , C07D317/62
CPC分类号： C07D317/62 , C07D303/36
摘要： In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
摘要翻译：在制备其中被保护的氨基醛与卤代甲基有机金属试剂在合适的溶剂中在-80℃以上反应的方法中，其中所述卤代甲基有机金属试剂是由有机金属试剂和二卤代甲烷之间的反应形成的，改进包括将保护的氨基醛流入保持在低于0℃的混合区，同时使所述混合区中的卤代甲基有机金属试剂流动，以使所述混合区与所述受保护的氨基醛接触，并且还从所述混合区抽出反应产物所述保护的氨基醛和所述卤代甲基有机金属试剂。

7. 发明授权

US4785124A Process for preparing higher order cuprate complexes 失效
标题翻译：制备高级铜酸盐络合物的方法
公开(公告)号：US4785124A
公开(公告)日：1988-11-15
申请号：US59294
申请日：1987-06-08
申请人： Arthur L. Campbell , James R. Behling , Sau-hoi N. John , Kevin A. Babiak
发明人： Arthur L. Campbell , James R. Behling , Sau-hoi N. John , Kevin A. Babiak
IPC分类号： C07F1/08 , C07F7/22
CPC分类号： C07F7/2212 , C07F1/08
摘要： This invention encompasses a process for preparing higher order cuprate complexes which contain a carbanion for the formation of carbon to carbon bonds in reactions such as epoxide addition. The complex is formed by reacting a first cuprate complex with a stannane such that the carbanion to be used to form carbon to carbon bonds is transferred from the stannane to the first cuprate complex to form a different higher order cuprate complex. This process permits the in situ preparation of a higher order cuprate complex having the carbanion desired to be used in a synthetic reaction. Higher order cuprate complexes derived from the reaction of a cuprate complex with 1,2-bis-tri-n-butylstannyl ethylene are particularly useful for the addition to epoxides to form vinyl tin intermediates useful for preparing omega side chains of prostaglandins.

8. 发明授权

US4661592A 4H-pyrimido[2,1-a]isoquinolin-4-one derivatives 失效
标题翻译： 4H-嘧啶并[2,1-a]异喹啉-4-酮衍生物
公开(公告)号：US4661592A
公开(公告)日：1987-04-28
申请号：US625061
申请日：1984-06-27
申请人： Arthur L. Campbell , Suzanne Evans Radak , Melanie J. Loots
发明人： Arthur L. Campbell , Suzanne Evans Radak , Melanie J. Loots
IPC分类号： A61K31/505 , A61P3/04 , A61P39/02 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to a class of novel 4H-pyrimido[2,1-a]isoquinoline derivatives. The invention further relates to pharmaceutical compositions containing such 4H-pyrimido[2,1-a]isoquinoline-4-one derivatives and to the use of such compounds and compositions as anorectic agents. In particular, the novel 4H-pyrimido[2,1-a]isoquinoline-4-one derivatives are effective anorectic agents when administered orally.
摘要翻译：本发明涉及一类新的4H-嘧啶并[2,1-a]异喹啉衍生物。本发明还涉及含有这样的4H-嘧啶并[2,1-a]异喹啉-4-酮衍生物的药物组合物，以及这些化合物和组合物作为厌食剂的用途。特别地，当口服给药时，新的4H-嘧啶并[2,1-a]异喹啉-4-酮衍生物是有效的厌食剂。

9. 发明授权

US5011958A Process for preparing higher order cuprate complexes 失效
标题翻译：制备高级铜酸盐络合物的方法
公开(公告)号：US5011958A
公开(公告)日：1991-04-30
申请号：US427067
申请日：1989-10-25
申请人： Arthur L. Campbell , James R. Behling , John S. Ng , Kevin A. Babiak
发明人： Arthur L. Campbell , James R. Behling , John S. Ng , Kevin A. Babiak
IPC分类号： C07F1/08 , C07F7/22
CPC分类号： C07F1/08 , C07F7/2212
摘要： This invention encompasses a process for preparing higher order cuprate complexes which contain a carbanion for the formation of carbon to carbon bonds in reactions such as epoxide addition. The complex is formed by reacting a first cuprate complex with a stannane such that the carbanion to be used to form carbon to carbon bonds is transferred from the stannane to the first cuprate complex to form a different higher order cuprate complex. This process permits the in situ preparation of a higher order cuprate complex having the carbanion desired to be used in a synthetic reaction. Higher order cuprate complexes derived from the reaction of a cuprate complex with 1,2-bis-tri-n-butylstannyl ethylene are particularly useful for the addition to epoxides to form vinyl tin intermediates useful for preparing omega side chains of prostaglandins.
摘要翻译：本发明包括一种制备高级铜酸盐配合物的方法，其中含有用于在诸如环氧化物添加的反应中形成碳 - 碳键的碳负离子。络合物通过使第一铜酸盐络合物与锡烷反应形成，使得用于形成碳 - 碳键的碳负离子从锡烷转移到第一铜酸盐络合物以形成不同的高级铜酸盐络合物。该方法允许原位制备具有期望在合成反应中使用的碳负离子的高级铜酸盐络合物。衍生自铜酸盐络合物与1,2-双 - 三正丁基甲锡烷基乙烯反应的高级铜酸盐络合物特别可用于加入环氧化物以形成可用于制备前列腺素的ω侧链的乙烯基锡中间体。

10. 发明授权

US4952724A Process for preparation of alpha-aryloxy acetic acids and their salts 失效
标题翻译： α-芳氧基乙酸及其盐的制备方法
公开(公告)号：US4952724A
公开(公告)日：1990-08-28
申请号：US447740
申请日：1989-12-08
申请人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A, Partis
发明人： Arthur L. Campbell , Richard A. Mueller , John S. Ng , Richard A, Partis
IPC分类号： C07C51/367 , C07C59/70
CPC分类号： C07C51/367
摘要： A process for producing aryloxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R-OH wherein R is aryl or substituted aryl with a base in an aprotic organic solvent to give an aryloxide followed by removal of the organic solvent and reaction of the aryloxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding aryloxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the aryloxyacetate salt with an acid.

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