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1. 发明授权

US4613460A Process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester 失效
标题翻译：制备α-L-天冬氨酰-L-苯丙氨酸甲酯的方法
公开(公告)号：US4613460A
公开(公告)日：1986-09-23
申请号：US661390
申请日：1984-10-16
申请人： Paolo Casati , Biagio Elefante , Claudio Fuganti
发明人： Paolo Casati , Biagio Elefante , Claudio Fuganti
IPC分类号： C07K1/113 , C07K5/075 , C07K5/06
CPC分类号： C07K5/0613
摘要： A process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester: ##STR1## in which: (a) the compound methyl N(.alpha.-L-aspartyl).alpha.-aminocinnamate, protected at the nitrogen, of formula: ##STR2## where R is a protector group at the nitrogen, is subjected to hydrogenation at the olefin bond by means of gaseous hydrogen in the presence of a hydrogenation catalyst, to give the compound of formula: ##STR3## where R has the aforesaid meaning, in the form of a mixture of .alpha.-L-aspartyl-L-phenylalanine methyl ester protected at the nitrogen, and .alpha.-L-aspartyl-D-phenylalanine methyl ester protected at the nitrogen;(b) the protector group is removed from the .alpha.-L-aspartyl-L-phenylalanine and .alpha.-L-aspartyl-D-phenylalanine methyl esters protected at the nitrogen;(c) the .alpha.-L-aspartyl-L-phenylalanine methyl ester is separated and recovered from the deprotection reaction product.
摘要翻译：制备α-L-天冬氨酰基-L-苯丙氨酸甲酯的方法：其中：（a）在氮保护下的式（A）化合物甲基N（α-L-天冬氨酰基）α-氨基肉桂酸酯：其中R是氮的保护基，在氢化催化剂存在下，通过气态氢在烯烃键上进行氢化，得到下式的化合物：（IV））其中R具有上述含义，以氮保护的α-L-天冬氨酰基-L-苯丙氨酸甲酯和氮保护的α-L-天冬氨酰-D-苯丙氨酸甲酯的混合物形式; （b）保护基团从α-L-天冬氨酰基-L-苯丙氨酸和α-L-天冬氨酰-D-苯丙氨酸甲酯在氮气保护下除去; （c）从脱保护反应产物中分离并回收α-L-天冬氨酰基-L-苯丙氨酸甲酯。

2. 发明授权

US4664852A Process for the preparation of L-carnitine 失效
标题翻译：制备左旋肉碱的方法
公开(公告)号：US4664852A
公开(公告)日：1987-05-12
申请号：US866144
申请日：1986-05-22
申请人： Paolo Casati , Claudio Fuganti
发明人： Paolo Casati , Claudio Fuganti
IPC分类号： C07C69/675 , C07C20060101 , C07C67/00 , C07C227/00 , C07C227/08 , C07C227/18 , C07C229/22 , C07C231/00 , C07C231/04 , C07C231/12 , C07C235/12 , C07C235/80 , C07C101/12
CPC分类号： C07C229/22
摘要： A process for preparing L-carnitine (I) wherein(a) diketene (II) is reacted with chlorine, and the chlorination product thus obtained is submitted to amidation by the methylester of an optically-active aminoacid, having formula: ##STR1## wherein R=CH.sub.2 A.sub.r or A.sub.r wherein Ar is a substituted or not-substituted aromatic group, to yield the compound 4-chloro-3-ketobutyrylamide of the methylester of the optically-active aminoacid: (IV)(b) the compound (IV) is reduced in the presence of a reducing agent to yield a mixture (V) of (3R)-4-chloro-3-hydroxybutyrylamide of the methylester of an optically-active acid (VI), and (3S)-4-chloro-3-hydroxybutyrylamide of the methylester of an optically active aminoacid (VII),(c) the compound (VI) is separated and recovered from the reduction reaction product,(d) the compound (VI) is submitted to methanolysis by hydrogen chloride gas in methanol,(e) the methylester of the optically-active aminoacid (III) is precipitated and recovered from the methanolysis reaction product,(f) from the mother liquors the methylester of (3R)-4-chloro-3-hydroxybutyric acid (VIII) is recovered,(g) the compound (VIII) thus obtained is treated with trimethylamine in ethanol, is hydrolyzed with hydrochloric acid and L-carnitine is separated and recovered.
摘要翻译：一种制备左旋肉碱（I）的方法，其中（a）双烯酮（II）与氯反应，由此获得的氯化产物经过具有下式的光学活性氨基酸的甲酯进行酰胺化： III）其中R = CH 2 Ar或Ar，其中Ar是取代或未取代的芳族基团，得到光学活性氨基酸的甲酯的化合物4-氯-3-酮丁酰胺：（IV）（b）化合物（ IV）在还原剂存在下还原，得到光学活性酸（VI）的甲酯的（3R）-4-氯-3-羟基丁酰胺的混合物（V），和（3S）-4- 光学活性氨基酸（VII）的甲酯的氯-3-羟基丁酰胺，（c）化合物（VI）从还原反应产物中分离回收，（d）化合物（VI）通过氯化氢进行甲醇分解在甲醇中的气体，（e）光学活性氨基酸（III）的甲酯沉淀并从甲烷中回收（f）从母液中回收（3R）-4-氯-3-羟基丁酸（VIII）的甲酯，（g）将所得化合物（Ⅷ）用乙醇中的三甲胺处理，用盐酸水解并分离和回收L-肉碱。

3. 发明授权

US08519160B2 Process for the preparation of rotigotine 有权
标题翻译：罗替戈汀的制备方法
公开(公告)号：US08519160B2
公开(公告)日：2013-08-27
申请号：US13120682
申请日：2009-09-24
申请人： Aldo Banfi , Gialunca Belogi , Claudio Fuganti , Roberta Pizzocaro
发明人： Aldo Banfi , Gialunca Belogi , Claudio Fuganti , Roberta Pizzocaro
IPC分类号： C07D333/20
CPC分类号： C07D333/08 , C07C211/38 , C07C213/08 , C07C215/64 , C07C2602/10 , C07D333/20
摘要： A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid-sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II). The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-1-methoxynaphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.
摘要翻译：制备罗替戈汀（I）及其药学上可接受的盐的方法，其包括用2-噻吩基乙酸 - 硼氢化钠络合物还原胺化式6的胺并使用氢溴酸盐5作为中间体（ II）。该方法从工业观点来看是有利的，因为它允许从光学活性5,6,7,8-四氢-6-（S）-N-丙基氨基-1-甲氧基萘（2）开始获得具有高对映体纯度的罗替高汀），避免使用危险的反应物，难以进行色谱分离或形成副产物。此外，公开了两种新的结晶形式。

4. 发明授权

US07816566B2 p-Menthan-3-ol alkylated derivatives and their use as refreshing agents 有权
标题翻译：对 - 薄荷醇-3-醇烷基化衍生物及其作为清爽剂的用途
公开(公告)号：US07816566B2
公开(公告)日：2010-10-19
申请号：US11579654
申请日：2005-04-28
申请人： Daniel Joulain , Claudio Fuganti , Stefano Serra , Andrea Vecchione
发明人： Daniel Joulain , Claudio Fuganti , Stefano Serra , Andrea Vecchione
IPC分类号： C07C35/08 , C07C35/12 , A61K8/18
CPC分类号： C07C35/08 , A23L27/203 , A61K8/345 , A61K2800/244 , A61Q9/02 , A61Q11/00 , A61Q13/00 , A61Q15/00 , A61Q19/00 , A61Q19/002 , C11B9/0015
摘要： The invention concerns a 3-alkylated crystallized (1R,4S)-p-menthan-(3)-ol derivative, of formula A or B, wherein: either when R represents hydrogen or a methyl radical, R represents a —(CH2)n-OH where n can be 1, 2 and 3, or when R represents a hydroxy radical, R represents a methyl radical or a —(CH2)n-OH group where n can be 1, 2 and 3. The invention also concerns methods for preparing same, and perfume, cosmetic or food compositions containing said derivative.
摘要翻译：本发明涉及式A或B的3-烷基化结晶（1R，4S） - 对 - （3） - 醇衍生物，其中：当R 2表示氢或甲基时，R 1，表示 - （CH 2）n -OH，其中n可以是1,2和3，或当R 2表示羟基时，R 1表示甲基或 - （CH 2）n -OH基团，其中n 本发明还涉及制备方法，以及包含所述衍生物的香料，化妆品或食品组合物。

5. 发明授权

US5527693A Process for the preparation of saturated delta-decanolide or delta-dodecanolide by biohydrogenation 失效
标题翻译：通过生物氢化制备饱和的δ-癸内酯或δ-十二烷醇酯的方法
公开(公告)号：US5527693A
公开(公告)日：1996-06-18
申请号：US391480
申请日：1995-02-21
申请人： Rosanna Cardillo , Claudio Fuganti , Massimo Barbeni , Gianna Allegrone
发明人： Rosanna Cardillo , Claudio Fuganti , Massimo Barbeni , Gianna Allegrone
IPC分类号： C07D309/30 , A23L27/20 , A23L27/24 , C12P17/06 , C12P17/08 , C12R1/645 , C12R1/78 , C12R1/84 , C12R1/85 , C12P1/02 , C12P7/42
CPC分类号： C12P17/06 , A23L27/2052 , A23L27/24
摘要： The production of natural delta-decanolide and/or delta-dodecanolide or mixtures thereof, by means of the biohydrogenation of a substrate containing the corresponding unsaturated lactones, delta-decen-2-olide and delta-dodecen-2-olide, respectively, and mixtures thereof, is performed by means of the use of a microorganism chosen from the group consisting of Saccharomyces delbrueckii, Pichia ohmeri, Hansenula anomala, Pichia stipitis, Debaromyces hansenii, Zymomonas mobilis, Zygosaccharomyces rouxii, Schawnniomyces occidentalis, Sarcina lutea and Geotrichum candidum.
摘要翻译：通过分别含有相应的不饱和内酯，δ-癸烯-2-醇和δ-十二碳烯-2-醇的底物的生物氢化，分别生产天然的δ-癸内酯和/或δ-十二烷醇内酯或其混合物，以及其混合物通过使用选自以下的微生物：德氏酵母酵母（Saccharomyces delbrueckii），欧洲毕赤酵母（Pichia ohmeri），汉逊酵母（Hansenula anomala），毕赤酵母（Desiromyces hansenii），运动发酵单胞菌（Zymomonas mobilis），罗霍氏菌（Zygosaccharomyces rouxii），西葫芦西葫芦（Schawnniomyces occidentalis）以及白纹兰土（Geotrichum candidum））。

6. 发明授权

US07553978B2 Process for the preparation of 1-naphthol mixed ethers and intermediates of crystalline forms of (+) and (−)-duloxetine 失效
标题翻译：（+）和（ - ） - 度洛西汀的结晶形式的1-萘酚混合醚和中间体的制备方法
公开(公告)号：US07553978B2
公开(公告)日：2009-06-30
申请号：US12090619
申请日：2006-10-13
申请人： Samuele Frigoli , Claudio Fuganti , Roberta Pizzocaro
发明人： Samuele Frigoli , Claudio Fuganti , Roberta Pizzocaro
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed.
摘要翻译：本发明涉及度洛西汀（1a）的制备方法，该方法包括1-氟萘与3-N，N-二甲基氨基-1-（2-噻吩基） - 丙-1-醇的反应， 3-二甲基-2-氧代 - 六氢嘧啶（DMPU）作为溶剂; 还公开了用于鉴别度洛西汀对映体并测定其光学纯度的方法。

7. 发明申请

US20090163733A1 P-menthan-3-ol alkylated derivatives and their use as refreshing agents 有权
标题翻译： P-薄荷醇-3-醇烷基化衍生物及其作为清爽剂的用途
公开(公告)号：US20090163733A1
公开(公告)日：2009-06-25
申请号：US11579654
申请日：2005-04-28
申请人： Daniel Joulain , Claudio Fuganti , Stefano Serra , Andrea Vecchione
发明人： Daniel Joulain , Claudio Fuganti , Stefano Serra , Andrea Vecchione
IPC分类号： C07C35/12 , C07C43/115 , C07C69/96
CPC分类号： C07C35/08 , A23L27/203 , A61K8/345 , A61K2800/244 , A61Q9/02 , A61Q11/00 , A61Q13/00 , A61Q15/00 , A61Q19/00 , A61Q19/002 , C11B9/0015
摘要： The invention concerns a 3-alkylated crystallized (1R,4S)-p-menthan-(3)-ol derivative, of formula A or B, wherein: either when R represents hydrogen or a methyl radical, R represents a —(CH2)n-OH where n can be 1, 2 and 3, or when R represents a hydroxy radical, R represents a methyl radical or a —(CH2)n-OH group where n can be 1, 2 and 3. The invention also concerns methods for preparing same, and perfume, cosmetic or food compositions containing said derivative.
摘要翻译：本发明涉及式A或B的3-烷基化结晶（1R，4S） - 对 - （3） - 醇衍生物，其中：当R 2表示氢或甲基时，R 1，表示 - （CH 2）n -OH，其中n可以是1,2和3，或当R 2表示羟基时，R 1表示甲基或 - （CH 2）n -OH基团，其中n 本发明还涉及制备方法，以及包含所述衍生物的香料，化妆品或食品组合物。

8. 发明申请

US20080287693A1 Process for the Preparation of 1-Naphthol Mixed Ethers and Intermediates of Crystalline Forms of (+) and (-)-Duloxetine 失效
标题翻译：（+）和（ - ） - 度洛西汀的结晶形式的1-萘酚混合醚和中间体的制备方法
公开(公告)号：US20080287693A1
公开(公告)日：2008-11-20
申请号：US12090619
申请日：2006-10-13
申请人： Samuele Frigoli , Claudio Fuganti , Roberta Pizzocaro
发明人： Samuele Frigoli , Claudio Fuganti , Roberta Pizzocaro
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed.
摘要翻译：本发明涉及度洛西汀（1a）的制备方法，该方法包括1-氟萘与3-N，N-二甲基氨基-1-（2-噻吩基） - 丙-1-醇的反应， 3-二甲基-2-氧代 - 六氢嘧啶（DMPU）作为溶剂; 还公开了用于鉴别度洛西汀对映体并测定其光学纯度的方法。

9. 发明授权

US07273937B2 Process for the preparation of Tazarotene 有权
标题翻译：扎扎罗汀制备方法
公开(公告)号：US07273937B2
公开(公告)日：2007-09-25
申请号：US11368486
申请日：2006-03-07
申请人： Samuele Frigoli , Claudio Fuganti , Stefano Serra , Francesco Pizzocaro , Angelo Bedeschi , Paolo Tubertini
发明人： Samuele Frigoli , Claudio Fuganti , Stefano Serra , Francesco Pizzocaro , Angelo Bedeschi , Paolo Tubertini
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： Tazarotene is prepared by deoxygenation of the corresponding S-oxide, in turn obtained according to two alternative synthetic pathways.
摘要翻译：他扎罗汀是通过相应的S-氧化物的脱氧制备的，依次由两种替代合成途径获得。

10. 发明授权

US5441874A Method for the acylation of the 7-amino group of the cephalosporanic ring 失效
标题翻译：头孢菌素环的7-氨基酰化方法
公开(公告)号：US5441874A
公开(公告)日：1995-08-15
申请号：US86849
申请日：1993-07-07
申请人： Maurizio Zenoni , Claudio Fuganti
发明人： Maurizio Zenoni , Claudio Fuganti
IPC分类号： C07D501/20 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/34 , C07D501/36 , C12P35/00 , C12P35/04
CPC分类号： C12P35/04 , C07D501/00 , Y02P20/55
摘要： A method for the acylation of the 7-amino group of the cephalosporanic ring, according to which a 7-ACA amino thiazolyl protected adduct is prepared by acylating said amino group by an aminothiazolyl acetic acid whose amino group has been protected by a phenyl acetyl or a phenoxy acetyl group, the amino group being then deprotected by aqueous hydrolysis in the presence of penicillin G amidase or respectively penicillin V amidase.
摘要翻译：酰基化头孢菌素环的7-氨基的方法，根据该方法，通过用氨基噻唑乙酸酰化所述氨基来制备7-ACA氨基噻唑基保护的加合物，其氨基已被苯基乙酰基或苯氧基乙酰基，然后在青霉素G酰胺酶或分别为青霉素V酰胺酶的存在下，通过水解水解脱氨基。

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