专利号:US-11661406-B2 优先权日:2018-08-13 标 题 :Method for producing intermediate useful for synthesis of SGLT inhibitor 发明人:LI QING RI; YOON HEE KYOON 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.
专利号:US-5118853-A 优先权日:1988-10-13 标题:Processes for the synthesis of 3-disubstituted aminoacroleins 发明人:LEE GEORGE T; REPIC OLJAN 权利人:SANDOZ LTD 摘要:Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II, n wherein n R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 1b is phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n one of R 3 and R 4 is ##STR11## and the other is primary or secondary C 1-6 alkyl not containing an asymmetric carbon atom, C 3-6 cycloalkyl or phenyl-(CH 2 ) m -, n wherein n R 7 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 8 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 9 is hydrogen, C 1-2 alkyl, C 1-2 alkoxy, fluoro or chloro, and n m is 1, 2 or 3, with the provisos that not more than one of R 7 and R 8 is trifluoromethyl, not more than one of R 7 and R 8 is phenoxy, and not more than one of R 7 and R 8 is benzyloxy, n R 5 is hydrogen, C 1-3 alkyl, n-butyl, i-butyl, t-butyl, C 3-6 cycloalkyl, C 1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, and n R 6 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, or benzyloxy, with the provisos that not more than one of R 5 and R 6 is trifluoromethyl, not more than one of R 5 and R 6 is phenoxy, and not more than one of R 5 and R 6 is benzyloxy, n R 10 is C 1-6 alkyl, each X is chloro or bromo, and each X.sup.⊖ is chloride or bromide.
专利号:US-10253153-B2 优先权日:2015-04-24 标题 :Linker and support for solid phase synthesis of nucleic acid, and production method of nucleic acid using said support 发明人:MAETA ERI; MORI KENJIRO; HORIE SHOHEI; ITO TAKAHIKO; SAITO SHOICHIRO; NAGAO RYUHEI 权利人:NITTO DENKO CORP 摘要:The present invention provides a linker for solid phase synthesis of nucleic acid, which consists of a compound represented by the formula (I) or the formula (II), a support for solid phase synthesis of nucleic acid, which has a structure represented by the formula (III), and a production method of a nucleic acid, which uses the support: n nwherein each symbol is as defined in the SPECIFICATION.
专利号:US-5191087-A 优先权日:1991-07-24 标 题 :Process for the synthesis of 1,4-disubstituted pyrazoles 发明人:ALCARAZ JEAN-MARIE; LECACHEUR MARYSE; ROBIN YVES 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The present invention relates to a process for the synthesis of 1,4-disubstituted pyrazoles. A monosubstituted hydrazine is reacted with the product of reaction of an acetal with an N-substituted halomethyliminium salt, preferably N,N-dimethylchloromethyliminium chloride. n The 1,4-disubstituted pyrazoles are, in particular, important intermediates in the synthesis of herbicides or drugs.
专利号:US-5290946-A 优先权日:1988-10-13 标 题 :Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes 发明人:LEE GEORGE T; KAPA PRASAD K; REPIC OLJAN 权利人:SANDOZ LTD 摘要:A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R 1 R 2 N--CHO and CH 2 â• CH--O--R 10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R 1 is phenyl or substituted phenyl or intermediates in the synthesis of the compounds of formula I which intermediates have the formula ##STR3## wherein R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n R 10 is C 1-6 alkyl, n X.sup.⊖ is chloride or bromide, and n R 3 -R 6 are as defined in the specification. n The compounds of Formula II are intermediates in the synthesis of known HMB-CoA reductase inhibitors which inhibit the biosynthesis of cholesterol and are useful as antihyperchloesterolemic gents.
专利号:US-10633360-B2 优先权日:2014-12-23 标题 :Efficient process for the synthesis of alkoxy substituted benzaldehydes 发明人:MOHAPATRA Manoj Kumar; BENDAPUDI Ramamohanrao; MENACHERRY Paul Vincent; PAUL VINCENT 权利人:ANTHEA AROMATICS PRIVATE LTD 摘要:The present invention relates to the synthesis of alkoxy substituted benzaldehydes obtained from the corresponding alkoxy substituted benzenes. Alkoxy substituted benzaldehydes are products of broad commercial interest and are used as end products and intermediates in flavor and fragrance applications and pharmaceutical ingredients. For example, 3,4-methylendioxy-benzaldehyde (also known as heliotropin or piperonal) is used widely both as a end product and intermediate for the above mentioned applications. Other examples include 3,4-dimethoxybenzaldehyde, 3,4,5-trimethoxybenzaldehyde and 3,4-ethylenedioxybenzene which are intermediates in the synthesis of active pharmaceutical intermediates.
[参考文献]: Jisheng Zhang, Et Al. Redox Inactive Metal Ion Triggered N-Dealkylation By An Iron Catalyst With Dioxygen Activation: A Lesson From Lipoxygenases. Dalton Trans. 2015 Jun 7;44(21):9847-59.
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