CAS: 7379-35-3; 4-Chloropyridine Hydrochloride

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4-羟基吡啶置于4-二甲氨基吡啶,氯化亚砜,三光气体系中,化学反应 3.5H,以94%的收率获得产物4-氯吡啶盐酸盐
参考文献:氮杂氮杂戊烯的高效无磷氯化反应及其在一锅法药物合成中的应用
标题:氮杂氮杂戊烯的高效无磷氯化反应及其在一锅法药物合成中的应用
摘要:用碳酸二(三氯甲基)酯(btc)和socl 2氯化羟基氮杂芳烃已经通过与5重量%的4-二甲基氨基吡啶(dmap)作为催化剂回流而有效地进行.各种底物都可以高产率氯化.所获得的氯化氮杂芳烃可通过简单的后处理直接直接用于大规模的一锅合成.
DOI:10.1021/acs.Oprd.9B00407

专利信息

专利号:US-8633321-B2
优先权日:2009-09-24
标 题 :Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof
发明人：CHOY NAKYEN; SHAY JR JOHN J; SLEDESKI ADAM W
权利人:CHOY NAKYEN; SHAY JR JOHN J; SLEDESKI ADAM W; SANOFI AVENTIS US LLC
摘要:The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).

专利号:WO-2024061842-A1
优先权日:2022-09-19
标 题:Improved oligonucleotide synthesis
发明人：CREUSEN GUIDO; MINUTH MARCO; SAMSON DANIEL
权利人:BACHEM HOLDING AG
摘要:A method for the solid-phase synthesis of a target oligonucleotide OT is disclosed, wherein said method comprises a step of incubating a nucleoside or oligonucleotide, which is covalently linked to a solid support and comprises a backbone hydroxyl moiety protected by a di(p-methoxyphenyl)phenylmethyl (DMT) protecting group, with a deprotection mixture, thereby cleaving said protecting group from said nucleoside or oligonucleotide, wherein said deprotection mixture is a liquid composition comprising a solvent, a protic acid having a pKa equal to or smaller than 4, and at least one alcohol of Formula (D), wherein in RD-1 R,D-2 R,D-3 RD-4 and RD-5 are indepently of each other selected from the group consisting of H, OH, a e1-e6-alkyl group, O(C1-C6-aIkyl), C(O)(Ci-C6-alkyl), C(O)O(Ci-C6-alkyl), F, Cl, Br, I, and CN. Such a method does not only suppress depurination, but also results in an acceptable product yield.

专利号:US-6512125-B1
优先权日:1994-05-13
标 题 :Preparation of 1H-indol-1-amines
发明人：LEE THOMAS B; GOEHRING KEITH E
权利人:AVENTIS PHARMA INC
摘要:The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.

专利号:US-2006052532-A1
优先权日:2002-04-10
标 题 :Swellable, easily cross-linked, essentially linear polymers, and the use of the same in solid phase synthesis
发明人：RADEMANN JORG
权利人:RADEMANN JORG
摘要:The invention relates to a novel polymer compound, the use of the same and a method for solid phase synthesis using an inventive polymer compound. Said polymer compound comprises linear polymer chains of general formula [R—X]n, wherein R represents a hydrocarbon group and X represents a group comprising at least one heteroatom. The linear polymer chains are cross-linked with each other by means of linking groups.

专利号:WO-2011037947-A1
优先权日:2009-09-24
标题:Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof

专利号:US-2012184745-A1
优先权日:2009-09-24
标题:Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof