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31. 发明授权

US5162540A Process for the production of (+) biotin 失效
标题翻译：生产（+）生物素的方法
公开(公告)号：US5162540A
公开(公告)日：1992-11-10
申请号：US777914
申请日：1991-10-17
申请人： John McGarrity , Leander Tenud
发明人： John McGarrity , Leander Tenud
IPC分类号： C07D491/048 , C07D495/04
CPC分类号： C07D495/04
摘要： (3aS,6aR)-[(R)-(1-phenylethyl)-3,4-methoxybenzyl dihydro-1H-furo-[3,4-d]-imidazol-2,4(3H,3aH)-dione and 1H-furo-[3,4-d]-imidazol-2,4-(3H,3aH)-dione derivatives which are useful as intermediates for preparing (+) biotin, also known as vitamin H.
摘要翻译：（3aS，6aR） - [（R） - （1-苯乙基）-3,4-甲氧基苄基二氢-1H-呋喃并[3,4-d] - 咪唑-2,4（3H，3aH） - 二酮和1H - 呋喃并[3,4-d] - 咪唑-2,4-（3H，3aH） - 二酮衍生物，其可用作制备（+）生物素（也称为维生素H）的中间体。

32. 发明授权

US5144047A Process for the production of tetronic acid alkyl esters 失效
标题翻译：生产季铵酸酯的方法
公开(公告)号：US5144047A
公开(公告)日：1992-09-01
申请号：US554372
申请日：1990-07-19
申请人： Laurent Duc , John McGarrity
发明人： Laurent Duc , John McGarrity
IPC分类号： C07D307/60
CPC分类号： C07D307/60
摘要： Tetronic acid alkyl esters are produced at a higher temperature by a ring closure of 4-halo-3-alkoxy-2-butene carboxylic acids. The tetronic acid alkyl esters are reacted by in acid hydrolysis in tetronic acid.
摘要翻译：季戊酸烷基酯通过4-卤代-3-烷氧基-2-丁烯羧酸的闭环在更高的温度下生产。四氢酸烷基酯通过在酸性水解中在四氢酸中反应。

33. 发明授权

US5117003A Process for the production of (+) biotin 失效
标题翻译：生产（+）生物素的方法
公开(公告)号：US5117003A
公开(公告)日：1992-05-26
申请号：US271180
申请日：1989-01-10
申请人： John McGarrity , Leander Tenud
发明人： John McGarrity , Leander Tenud
IPC分类号： C07B61/00 , C07D233/32 , C07D307/00 , C07D491/048 , C07D495/04
CPC分类号： C07D495/04 , Y02P20/55
摘要： Process for the production of (+) biotin.

34. 发明授权

US4983744A Substituted thienylethylamines and process for their production 失效
标题翻译：取代的噻吩乙胺及其生产方法
公开(公告)号：US4983744A
公开(公告)日：1991-01-08
申请号：US469354
申请日：1990-01-24
申请人： Aleksander Warm , John McGarrity
发明人： Aleksander Warm , John McGarrity
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： Substituted thienylethylamines of the formula: ##STR1## wherein R is formyl, acetyl or benzoyl or is benzyl, which is ring-substituted by at least one halogen atom, and R.sub.1 is lower alkyl, phenyl or substituted phenyl, are initial products for the production of antithromobolytically effective pharmaceutical agents. A process for the production of the above-mentioned compounds from substituted ethanolamines by their reaction with strong bases, further reaction with the resultant aziridines with 2-thienyllithium, and conversion of the resultant thienylethylamines with compounds of formula RX, wherein R has the above-mentioned meaning and X is a halogen.

35. 发明授权

US4970325A Substituted thienylethylamines and process for their production 失效
标题翻译：取代的噻吩乙胺及其生产方法
公开(公告)号：US4970325A
公开(公告)日：1990-11-13
申请号：US418340
申请日：1989-10-06
申请人： Aleksander Warm , John McGarrity
发明人： Aleksander Warm , John McGarrity
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： Substituted thienylethylamines of the formula: ##STR1## wherein R is formyl, acetyl or benzoyl or is benzyl, which is ring-substituted by at least one halogen atom, and R.sub.1 is a lower alkyl, phenyl or substituted phenyl, are initial products for the production of antithrombolytically effective pharmaceutical agents. A process for the production of the above-mentioned compounds from substituted ethanolamines by their reaction with strong bases, further reaction with the resultant aziridines with 2-thienyllithium, and conversion of the resultant thienylethylamines with compounds of formula RX, wherein R has the above-mentioned meaning and X is a halogen.
摘要翻译：取代的下式的噻吩乙基胺：其中R是甲酰基，乙酰基或苯甲酰基，或是被至少一个卤素原子环取代的苄基，R 1是低级烷基，苯基或取代的苯基，是初始的产品用于生产抗血栓溶解有效的药剂。通过与强碱反应从取代的乙醇胺制备上述化合物的方法，与得到的氮丙啶与2-噻吩基锂的进一步反应，以及所得噻吩乙基胺与式RX化合物的转化，其中R具有上述结构，并且X是卤素。

36. 发明授权

US4876350A Process for the production of (+) biotin 失效
标题翻译：生产（+）生物素的方法
公开(公告)号：US4876350A
公开(公告)日：1989-10-24
申请号：US134210
申请日：1987-12-16
申请人： John McGarrity , Leander Tenud
发明人： John McGarrity , Leander Tenud
IPC分类号： C07B61/00 , C07D233/32 , C07D307/00 , C07D491/048 , C07D495/04 , C07D231/00
CPC分类号： C07D495/04 , Y02P20/55
摘要： Process for the production of (+) biotin. A compound of the formula: ##STR1## wherein R.sub.1 is e.g., an (R)-1-phenylalkyl group, and R.sub.2 is, e.g., hydrogen. The desired diastereomer of the formula: ##STR2## is separated out. If R.sub.2 is H, a protective group is introduced by reaction with, e.g., an aliphatic acid chloride. The diastereomer is converted by reaction with a thiocarboxylic acid salt derivative into the corresponding thiolacetone, which is reacted with a Grignard reactant and subsequently water is split off. Alternatively, the corresponding thiolacetone is reacted with a compound of the formula:(C.sub.6 H.sub.5).sub.3 P.sup..sym. (CH.sub.2).sub.4 COOR.sub.3.X.sup..crclbar.wherein R.sub.3 is, e.g., H, and X is a halogen atom, in the presence of a base to provide a compound of the formula: ##STR3## Such compound is catalytically hydrogenated and then converted into (+) biotin by cleavage of the protective groups.
摘要翻译：生产（+）生物素的方法。下式的化合物：其中R 1是例如（R）-1-苯基烷基，R 2是例如氢。分离出所需的下式的非对映异构体：。如果R 2为H，则通过与例如脂族酰氯反应引入保护基。通过与硫代羧酸盐衍生物的反应将非对映异构体转化成相应的硫醇丙酮，其与格氏反应物反应，随后将水分离。或者，相应的硫醇丙酮与下式化合物（C6H5）3P（+）（CH2）4COOR3X（ - ）反应，其中R3为例如H，X为卤素原子，在碱以提供下式的化合物：该化合物被催化氢化，然后通过保护基团的裂解转化成（+）生物素。

37. 发明授权

US4824966A Process for the production of 4-hydroxy-2-oxo-pyrrolidin-1-yl acetamide 失效
标题翻译：制备4-羟基-2-氧代 - 吡咯烷-1-基乙酰胺的方法
公开(公告)号：US4824966A
公开(公告)日：1989-04-25
申请号：US188702
申请日：1988-05-04
申请人： Thomas Meul , John McGarrity
发明人： Thomas Meul , John McGarrity
IPC分类号： C07D207/38 , C07D207/27
CPC分类号： C07D207/38
摘要： Process for the production of 4-hydroxy-2-oxo-pyrrolidin-1-yl acetamide. A 4-(C.sub.1 -C.sub.2)-alkoxy-3-pyrrolin-2-on-1-yl-acetic acid (C.sub.1 -C.sub.4)-alkyl ester of the formula: ##STR1## wherein R.sub.1 is alkyl having 1 or 2 C atoms and R.sub.2 is alkyl having 1 to 4 C atoms, is reacted with either trichloromethylsilane in the presence of an alkali iodide or in an acid anhydrous medium to a 2,4-dioxo-pyrrolidin-1-yl-acetic acid (C.sub.1 -C.sub.4)-alkyl ester. The latter is optionally isolated and then hydrogenated with sodium borohydride to a 4-hydroxy-2-oxo-pyrrolidin-1-yl-acetic acid (C.sub.1 -C.sub.4)-alkyl ester. Finally, the 4-hydroxy-2-oxo-pyrrolidin-1-yl-acetic acid (C.sub.1 -C.sub.4)-alkyl ester is converted by amidation with ammonia to the desired end product.
摘要翻译：制备4-羟基-2-氧代 - 吡咯烷-1-基乙酰胺的方法。具有下式的4-（C 1 -C 2） - 烷氧基-3-吡咯烷-2-酮-1-基 - 乙酸（C 1 -C 4） - 烷基酯，其中R 1是具有1或2个C原子的烷基 R2是具有1-4个碳原子的烷基，在碱金属碘化物存在下或在酸性无水介质中与三氯甲基硅烷反应成2,4-二氧代 - 吡咯烷-1-基 - 乙酸（C 1 -C 4） - 烷基酯。后者任选地分离，然后用硼氢化钠氢化成4-羟基-2-氧代 - 吡咯烷-1-基 - 乙酸（C 1 -C 4） - 烷基酯。最后，通过用氨的酰胺化将4-羟基-2-氧代 - 吡咯烷-1-基 - 乙酸（C 1 -C 4） - 烷基酯转化为所需的最终产物。

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