专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-7323575-B2 优先权日:2003-04-09 标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid 发明人:SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.
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-5623068-A 优先权日:1994-03-07 标 题:Synthesis of DNA using substituted phenylacetyl-protected nucleotides 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; HANNA NAEEM B 权利人:BECKMAN INSTRUMENTS INC 摘要:Deoxyribonucleotide and ribonucleotide derivatives of the general formula I I wherein R1 represents -CR'R''-Ar, in which Ar is substituted aryl (as hereinafter defined) and R' and R'' are independently selected from the group consisting of hydrogen and lower alkyl; one of -R2 and R3 is a hydroxyl-protecting group and the other is a group suitable for synthesis of polynucleotides or for attachment of the nucleotide to a solid support; R4 is selected from the group consisting of hydrogen, -OH and protected hydroxyl; and B represents a divalent radical corresponding to a purine or pyrimidine base. When synthesis is carried out using these derivatives, the deprotection procedure is reduced to an essentially instantaneous process. The derivatives have acceptable shelf life and are very stable to conventional DNA synthesis conditions. Particularly preferred are those compounds wherein Ar is mono- and dihalo-substituted phenyl.
专利号:WO-2025134140-A1 优先权日:2023-12-19 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; SHAH JIGARKUMAR HARKISHANDAS; KALE MANOJ GANPAT; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of compounds of formula (I) or a salt thereof, wherein, R is selected from hydrogen, halogen, cyano, C1-C12 alkyl, C1-C12 haloalkyl, C1-C12 alkoxy, C1-C12 haloalkoxy, or C3-C8 cycloalkyl; R4 is selected from hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C1-C12 haloalkyl, C2-C12 haloalkenyl, C2-C12 haloalkynyl, C1-C12 alkoxy, C1-C12 haloalkoxy, C3-C8 cycloalkyl, or C3-C8 cycloalkyl-C1-C10 alkyl; and n represents an integer selected from 0-4. The method further comprises the synthesis of an anthranilic diamide compound of formula (A).
专利号:WO-2025057193-A1 优先权日:2023-09-13 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; KALE MANOJ GANPAT; SHAH JIGARKUMAR HARKISHANDAS; GAVHANE KISHOR BAPU; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention provides a method for the synthesis of compounds of formula (I), intermediates, and salts thereof, formula (I) wherein, R, R1 and n are as described in the description. The method further comprises the synthesis of anthranilic diamide compounds of formula (E), wherein the formula (E) is described in the description.
1: Nardini V, Palaretti V, Dias LG, da Silva GVJ. An Explanation about the Use of (S)-Citronellal as a Chiral Derivatizing Agent (CDA) in (1)H and (13)C NMR for Sec-Butylamine, Methylbenzylamine, and Amphetamine: A Theoretical-Experimental Study. Molecules. 2019 Aug 3;24(15). pii: E2830. doi: 10.3390/molecules24152830. 2: Douša M. Enantioseparation of N-acetyl-dl-cysteine as o-phtaldialdehyde derivatives obtained with various primary aliphatic amine additives on polysaccharide-based chiral stationary phases. J Pharm Biomed Anal. 2019 Mar 20;166:147-154. doi: 10.1016/j.jpba.2019.01.006. Epub 2019 Jan 8. Chinese. doi: 10.1039/c0cc03585h. Epub 2011 Jan 24. doi: 10.1002/jms.1464. Epub 2006 Dec 1. Epub 2005 Jul 8. Epub 2003 Nov 14. Chinese.
合成参考文献
参考文献:10.1107/s1600536811007513 摘要:Maharramov AM, Khalilov AN, Gurbanov AV, Allahverdiyev MA, Ng SW. 1-Methyl-amino-3-(2,4,6-trimethyl-phen-yl)propan-2-ol. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o784.