专利号:WO-2022269384-A1 优先权日:2021-06-24 标 题 :A process for the direct synthesis of fedratinib intermediate 发明人:DESAI ASIM HEMANTBHAI; PATIL SANJAY NIMBAJI; RADADIYA VAIBHAV GOVINDBHAI; DESAI JIGNASU THAKORBHAI; DUBEY RAJEEV RAMCHANDRA; CHOUBEY Ajit Kumar 权利人:AMI ORGANICS LTD 摘要:The present disclosure relates to a process for the direct synthesis of Fedratinib intermediate. Particularly, the present disclosure relates to a process for the direct synthesis of 3-amino-N- (tert-butyl)benzene sulfonamide. The process of the present disclosure has various advantages such as convenient operation conditions, time-saving process, easy purification, low operation costs, good yield and efficiency hence the process is industrially feasible. The use of non-toxic, inexpensive and easily available reagents, in the process of the present disclosure, makes the process cost-efficient economic and environmental friendly.
专利号:US-5326885-A 优先权日:1992-05-01 标 题 :Process of preparing enriched enantiomers of glycerol carbonate and derivatives thereof for synthesis of β-blockers 发明人:OLIVERO ALAN G; CASSEL JONATHAN M; POULSEN JAMES R 权利人:COGNIS INC 摘要:Enriched enantiomers of glycerol Carbonate are produced under the influence of a hydrolytic enzyme, either by selective esterification of racemic glycerol carbonate or by selective hydrolysis of an ester of the racemate. The enriched enantiomeric product is readily converted to starting materials and intermediates useful in the synthesis of enantiomerically pure therapeutic agents, such as beta -adrenergic blockers.
专利号:US-5223626-A 优先权日:1988-11-21 标 题:Preparation of cationic alkylenediamine dye intermediates 发明人:VINCZE JANOS; HERTER WILFRIED 权利人:CIBA GEIGY CORP 摘要:Compounds of the formula (1) where R1, R2 and R3 are each independently of the others hydrogen, C1-C4alkyl, C1-C4alkoxy, halogen or C1-C4alkanoylamino, R is hydrogen or unsubstituted or C1-C4alkoxy substituted C1-C12alkyl or an -(alk)-NA(+)X(-) radical or, R forms together with an R1 in the ortho-position relative to the amino group a partially hydrogenated, substituted or unsubstituted 5- to 7-membered heterocyclic ring which may contain additional N, S or O atoms as ring members, (alk) is a substituted or unsubstituted C1-C6alkylene radical, -NA(+) is the radical of an amino compound of formula (2) or (2') where R4, R5 and R6 are each independently of the others substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C7-C12aralkyl or substituted or unsubstituted aryl, R8 and R9 are each independently of the other substituted or unsubstituted C1-C6alkyl, and R10 and R11 are each independently of the other hydrogen, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C7-C12aralkyl or substituted or unsubstituted aryl, or is the positively charged radical of a 5- to 7-membered aliphatic or aromatic heterocycle which may contain additional N, S or O atoms as ring members, and X(-) is a halide ion, are prepared by reacting a compound of the formula (3) with a halogenating agent in the presence of a compound of the formula NA(2a) where the symbols are as defined in claim 1, these compounds being useful coupling components for the synthesis of cationic dyes.
专利号:US-7439364-B2 优先权日:2001-05-17 标 题 :Process for the synthesis of derivatives of halo-[2,3-F] quinoline 发明人:CHAN ANITA W; CURRAN TIMOTHY T; IERA SILVIO; CHEW WARREN; SELLSTEDT JOHN H; VID GALINA; FEIGELSON GREG; DING ZHIXIAN 权利人:WYETH CORP 摘要:Methods of preparing compounds of Formula I n nare provided.
专利号:US-4552984-A 优先权日:1982-01-21 标题 :Process for preparation of α,α-difluoroalkoxy or α,.alpha. 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl sulfones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a sulfonic acid, a derivative or a precursor of this acid, in the presence of boron trifluoride in an amount such that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-6943254-B2 优先权日:1997-03-07 标 题 :Synthesis of pyrazinyl pyridine-3-sulfonamide compounds 发明人:HOGAN PHILIP JOHN 权利人:ASTRAZENECA UK LTD 摘要:A process for the manufacture of: n n nwherein R is (1-4C)alkyl, carboxyl(1-4C)alkyl or 1,3,4-oxadiazol-2-yl comprises:n (a) reaction of the diazonium salt of 3-amino-2-chloropyridine with thionyl chloride in water and an electron transfer catalyst; (b) reaction with isobutyl-(3-methoxy-5-methylpyrazin-2-yl)carbamate and an alkali metal hydride in inert solvent; and (I) where R is (1-4C)alkyl, carboxy(1-4C)alkyl: (c) reaction with a boronic acid: n n (or an anhydride or ester therof) in the presence of a base and a palladium or nickel catalyst in solvent; and removal of the isobutoxy carbonyl group; or (ii) where R is 1,3,4-oxadiazol-2-yl (c) reaction with 4-methoxycarbonylphenylboronic acid (or an anhydride or ester thereof) with a source fluoride ion under aqueous conditions; (d) removal of the isobutoxycarbonyl protecting group; (e) conversion of the methyl ester group to the hydrazide; and (f) conversion to a 1,3,4-oxadiazol-2-yl moiety.
摘要:Shcherbakova, I., Science of Synthesis, (2007) 31, 807. 摘要:Rakitin, O. A., Science of Synthesis, (2007) 31, 1091. 摘要:Shcherbakova, I., Science of Synthesis, (2007) 31, 826.