公开(公告)号：US4724102A

公开(公告)日：1988-02-09

申请号：US844834

申请日：1986-03-27

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Mauro Morotti

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Mauro Morotti

IPC分类号： C07C59/64 ,  C07B31/00 ,  C07B57/00 ,  C07C51/00 ,  C07C51/06 ,  C07C51/487 ,  C07C67/00 ,  C07C235/34 ,  C07C87/30

CPC分类号： C07C51/06 ,  C07C51/487

摘要： A new process for the optical resolution of racemic mixtures of .alpha.-naphthylpropionic acids of formula ##STR1## wherein R.sub.1 is (C.sub.1-6) alkyl and R.sub.2 represents hydrogen or a halogen atom comprises reacting a racemic mixture of a compound of formula II ##STR2## wherein R.sub.1 and R.sub.2 have the above seen meanings and R.sub.3 is a reactive group, with an optically active aminoacid of formula ##STR3## wherein R.sub.4 represents a (C.sub.1-8) alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or carboxy, and m is an integer from 0 to 4, to give a pair of diastereoisomeric amides of formula ##STR4## wherein R.sub.1, R.sub.2, R.sub.4 and m have the above seen meanings, and M is a hydrogen atom or a cation of an alkali metal or a cation of an organic base. Compounds IV are resolved into the single diastereoisomeric amides d,d or 1,d, or d,1 or 1,1. Acid hydrolysis gives the optically active compound I.

摘要翻译： 用于光学拆分式（Ia）的α-萘基丙酸的外消旋混合物的新方法，其中R 1为（C 1-6）烷基且R 2表示氢或卤素原子包括使式II化合物的外消旋混合物 其中R 1和R 2具有上述的意义且R 3是反应性基团，其中式III的光学活性氨基酸其中R 4表示（C 1-8）烷基，苯基，取代的苯基，苄基，取代的苄基 或羧基，m为0至4的整数，得到一对式IV的非对映异构体酰胺，其中R 1，R 2，R 4和m具有上述含义，M为氢原子或 碱金属或有机碱的阳离子。 化合物IV被分解成单一非对映异构体酰胺d，d或1，d或d，1或1,1。 酸水解产生光学活性化合物I.

公开(公告)号：US4962223A

公开(公告)日：1990-10-09

申请号：US375131

申请日：1989-07-03

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Mauro Morotti

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Mauro Morotti

IPC分类号： C07C227/26 ,  C07C221/00 ,  C07C227/34 ,  C07C229/36 ,  C07C237/20 ,  C07C255/26 ,  C07C255/43 ,  C07C309/19

CPC分类号： C07C229/36 ,  C07C227/34 ,  C07C255/43

摘要： New process for the synthesis of the levodopa, L-(-)-2-amino-3-(3,4-dihydyphenyl)propionic acid, drug used in the treatment of the Parkinson's disease. The process consists in resolving with d-camphorsulfonic acid, or with a salt thereof, the d,l-2-amino-3-(3,4-dimethoxyphenyl)propionitrile, obtained from the 3,4-dimethoxyphenylacetaldehyde, and in the subsequent hydrolysis and demethylation, by means of concentrated solutions of haloid acids, of the d-2-amino-3-(3,4-dimethoxyphenyl)propionitrile and of salts thereof.

公开(公告)号：US5041637A

公开(公告)日：1991-08-20

申请号：US374769

申请日：1989-07-03

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Claudio Calzolari

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Claudio Calzolari

IPC分类号： C07B53/00 ,  C07C227/20 ,  C07C227/32 ,  C07C227/34 ,  C07C229/36 ,  C07C233/51 ,  C07C233/87 ,  C07C237/20 ,  C07C255/44 ,  C07C271/22

CPC分类号： C07C255/44 ,  C07C227/34 ,  C07C233/51 ,  C07C233/87 ,  C07C237/20 ,  C07C271/22

摘要： New process for the synthesis of optically active aminoacids of formula ##STR1## by treating compounds of formula ##STR2## which an optically active alcohol of formulaR.sub.4 --OH (III)d or 1To obtain a pair of diastereoiosmer esters of formula ##STR3## which is resolved in basic medium into the single diastereoisomer esters of formula ##STR4## from which the desired optically active aminoacid of formula (I) is obtained by treatment in acid medium.

公开(公告)号：US4661628A

公开(公告)日：1987-04-28

申请号：US668301

申请日：1984-11-05

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani

IPC分类号： C07C59/64 ,  C07B31/00 ,  C07B57/00 ,  C07C51/00 ,  C07C51/06 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C231/20 ,  C07C235/32 ,  C07C309/73 ,  C07C313/00 ,  C07C315/06 ,  C07C317/46 ,  C07C323/20 ,  C07C323/62 ,  C07D233/56 ,  C07C103/26 ,  C07C149/41 ,  C07D209/18 ,  C07D233/64

CPC分类号： C07C51/06

摘要： A new process for the optical resolution of racemic mixtures of .alpha.-naphthyl-propionic acids of formula ##STR1## This process comprises reacting a racemic mixture of a compound of formula ##STR2## with an optically active substance of formula R.sub.4 --NH.sub.2 (III), said substance being a .beta.-aminoalcohol, thus forming a pair of diastereoisomeric amides which are resolved into the single diastereoisomers by fractional crystallization. The obtained single diastereoisomeric amide is then hydrolyzed to give the desired optically active .alpha.-naphthyl-propionic acid of formula ##STR3## In the above compound I.fwdarw.III and VI, R.sub.1 is (C.sub.1-6)alkyl, R.sub.2 stands for hydrogen, halogen, mercapto, (C.sub.1-6)alkylthio, phenylthio, benzylthio, (C.sub.1-6)alkylsulfonyl, benzenesulfonyl, benzenesulfonyl substituted by halogen or (C.sub.1-4)alkyl, R.sub.3 is a reactive group and R.sub.4 is the residue of a primary or secondary alcohol.

摘要翻译： 用于光学拆分式（I）的α-萘基 - 丙酸的外消旋混合物的新方法该方法包括将式II化合物的外消旋混合物与式R4-NH2的光学活性物质 III），所述物质是β-氨基醇，从而形成一对非对映异构体酰胺，其通过分级结晶分解成单一非对映异构体。 然后将获得的单一非对映异构体酰胺水解，得到所需的式VI的光学活性α-萘基 - 丙酸在上述化合物I> III和VI中，R 1是（C 1-6）烷基，R 2代表氢 ，卤素，巯基，（C 1-6）烷硫基，苯硫基，苄硫基，（C 1-6）烷基磺酰基，苯磺酰基，被卤素或（C 1-4）烷基取代的苯磺酰基，R 3是反应性基团，R 4是伯 或仲醇。

公开(公告)号：US4622419A

公开(公告)日：1986-11-11

申请号：US795516

申请日：1985-11-06

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani

IPC分类号： C07B57/00 ,  C07B31/00 ,  C07C51/00 ,  C07C51/06 ,  C07C51/487 ,  C07C57/38 ,  C07C59/64 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C231/20 ,  C07C235/08 ,  C07C235/34 ,  C07C103/26

CPC分类号： C07C51/487

摘要： A process for the optical resolution of racemic mixtures of .alpha.-naphthyl-propionic acids of formula I ##STR1## which consists of reacting a racemic mixture of a compound of formula II ##STR2## with an optically active compound of formula IIIR.sub.4 --NH.sub.2wherein R.sub.4 is the residue of a primary or secondary alcohol which, taken with the NH.sub.2 radical, forms an optically active .beta.-aminoalcohol, to give a pair of diastereoisomeric amides, which is resolved into the single diastereoisomeric amides. Acid hydrolysis gives the optically active d or l .alpha.-naphthyl-propionic acids. The meaning of R.sub.1, R.sub.2, R.sub.3 is given.

摘要翻译： 用于光学拆分式I的α-萘基 - 丙酸的外消旋混合物的方法，其由式II化合物的外消旋混合物与式III的-NH-NH 2的光学活性化合物反应，其中 R4是伯或仲醇的残基，其与NH 2基团一起形成光学活性的β-氨基醇，得到一对非对映异构体酰胺，其被分解成单一非对映异构体酰胺。 酸水解得到光学活性的d或lα-萘基 - 丙酸。 给出了R1，R2，R3的含义。

公开(公告)号：US5107013A

公开(公告)日：1992-04-21

申请号：US634742

申请日：1990-12-27

申请人： Vincenzo Cannata ,  Claudio Calzolari ,  Giancarlo Tamerlani

发明人： Vincenzo Cannata ,  Claudio Calzolari ,  Giancarlo Tamerlani

IPC分类号： C07C45/46 ,  C07C45/65 ,  C07C51/377 ,  C07C69/734 ,  C07C231/12 ,  C07C255/37

CPC分类号： C07C255/37 ,  C07C231/12 ,  C07C45/46 ,  C07C45/65 ,  C07C51/377 ,  C07C69/734

摘要： Naphthalenes of formula ##STR1## wherein X represents COCH.sub.3, COC.sub.2 H.sub.5, CH(CH.sub.3)COOH, CH(CH.sub.3)COOR, CH(CH.sub.3)CN and CH(CH.sub.3)CONHR.sub.1, R represents alkyl and R.sub.1 represents hydrogen, alkyl or hydroxyalkyl, are debrominated by means of acceptors of bromine, like alkylarenes and alkoxyarenes, in the presence of Lewis acids.

公开(公告)号：US5097058A

公开(公告)日：1992-03-17

申请号：US512909

申请日：1990-04-25

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

IPC分类号： C07D301/02 ,  C07B61/00 ,  C07C45/00 ,  C07C45/58 ,  C07C47/277 ,  C07C67/00 ,  C07C239/00 ,  C07C249/08 ,  C07C251/36 ,  C07C251/40 ,  C07C253/00 ,  C07C255/37 ,  C07C255/53 ,  C07D303/48

CPC分类号： C07C255/00 ,  C07C45/58 ,  C07C47/277 ,  C07D303/48

摘要： New process for the synthesis of the .alpha.-(1-m.ethylethyl)-3,4-dimethoxyacetonitrile of formula (I): ##STR1## which is known as an intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the isobutyryl-3,4-dimethoxybenzene of formula (II): ##STR2## which, by means of the Darzens condensation, gives an epoxyester which, by alkaline hydrolysis and subsequent decarboxylation, gives the .alpha.-(1-methylethyl)-3,4-dimethoxybenzeneacetaldehyde. This product is reacted with hydroxylamine to obtain the corresponding oxime that, by dehydration, gives the nitrile of formula I.

公开(公告)号：US5057624A

公开(公告)日：1991-10-15

申请号：US502038

申请日：1990-03-30

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani ,  Graziano Zagnoni

IPC分类号： C07C213/04 ,  C07C213/00 ,  C07C213/02 ,  C07C217/60

CPC分类号： C07C213/02 ,  C07C217/60

摘要： New process for the synthesis of the N-methyl-3,4-dimetoxyphenylethylamine of formula ##STR1## intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the 3,4-dimethoxybenzaldehyde which, by means of a Darzens condensation, gives an epoxyester that, by alkaline hydrolysis and subsequent decarboxylation, gives the 3,4-dimethoxyphenylacetaldehyde. This aldehyde gives the amine of formula I by reaction with monomethylamine followed by reduction with sodium borohydride.

公开(公告)号：US4423244A

公开(公告)日：1983-12-27

申请号：US362679

申请日：1982-03-29

申请人： Vincenzo Cannata ,  Giancarlo Tamerlani

发明人： Vincenzo Cannata ,  Giancarlo Tamerlani

IPC分类号： C07C51/347 ,  B01J25/02 ,  B01J27/00 ,  B01J31/02 ,  C07B31/00 ,  C07B57/00 ,  C07B61/00 ,  C07C45/46 ,  C07C45/58 ,  C07C51/00 ,  C07C51/377 ,  C07C51/487 ,  C07C59/64 ,  C07C67/00 ,  C07C65/105

CPC分类号： C07C51/377 ,  C07C45/46 ,  C07C45/58 ,  C07C51/487

摘要： A new process for the preparation of the d-2-(6-methoxy-2-naphthyl)-propionic acid of formula ##STR1## which comprises resolving a racemic mixture of the d- and 1-2-(5-halo-6-methoxy-2-naphthyl)-propionic acids of formula ##STR2## wherein halo stands for a halogen atom, recovering the d-isomer and subjecting this isomer to catalytic dehalogenation. Compound I is obtained in very high yields and with a high purity degree.

摘要翻译： 对于d 2-（6-甲氧基-2-萘基）式的 - 丙酸我其包括解决的d的和1-2-的外消旋混合物（5-卤代的制备的新工艺 6-甲氧基-2-萘基）的式 - 丙酸 II，其中卤素代表卤原子，回收d-异构体和使该异构体以催化脱卤。 化合物I在非常高的产率和高纯度的程度而获得的。

公开(公告)号：US20120258166A1

公开(公告)日：2012-10-11

申请号：US13527399

申请日：2012-06-19

申请人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

发明人： Giuseppe Claudio Viscomi ,  Manuela Campana ,  Dario Braga ,  Donatella Confortini ,  Vincenzo Cannata ,  Paolo Righi ,  Goffredo Rosini

IPC分类号： A61K31/437 ,  A61K9/48 ,  A61P31/00 ,  C07D498/22

CPC分类号： C07D498/22

摘要： Forms of rifaximin (INN) antibiotic, such as the poorly crystalline form named rifaximin γ are described, along with the production of medicinal preparations containing rifaximin for oral and topical use.