CAS: 286961-14-6; Tert-Butyl 4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-5,6-Dihydropyridine-1(2H)-Carboxylate

相似化合物

844501-00-4 454482-11-2 286961-15-7

上下游产品

4-Trifluoromethanesulfonyloxy-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester bis(pinacol)diborane N-tert-butyloxycarbonylpiperidin-4-one bis(pinacolato)diborane4-(4-methoxyphenyl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester tert-butyl 4-(5-chloro-4-methyl-2-propionylphenyl)-3,6-dihydropyridine-1(2H)-carboxylate 4-[3-(isobutyrylamino)phenyl]-3,6-dihydro-1(2H)-pyridine carboxylic acid tert-butyl ester 4-(3-isobutyrylamino-2-methylphenyl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester

叔-丁基氯甲酸酯置于甲醇,4-二甲氨基吡啶,(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,Sodium Tetrahydroborate,Potassium Acetate体系中,用 甲苯,乙腈 用作溶剂,化学反应 4.0H,反应生成N-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯
参考文献:一种n-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯的合成新方法
标题:一种n-Boc-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯的合成新方法
摘要:本发明公开了一种n‑boc‑1,2,5,6‑四氢吡啶‑4‑硼酸频哪醇酯的合成新方法,包括以下三个反应步骤:以4‑溴吡啶盐酸盐为起始原料,首先与氯甲酸叔丁酯或二碳酸二叔丁酯反应制备4‑溴‑n‑boc‑氯化吡啶,再经nabh4还原制备n‑boc哌啶‑4‑烯基溴化合物,最后通过与联硼酸频哪醇酯发生偶联反应制备目标产物n‑boc‑1,2,5,6‑四氢吡啶‑4‑硼酸频哪醇酯.该合成路线,原料易得,条件温和,副产少,收率高,较适合于工业化放大.

专利信息

专利号:US-8901304-B1
优先权日:2013-11-05
标题:Benzo[D]imidazole derivatives of piperidine and piperazine
发明人：ULLAH NISAR
权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH
摘要:The benzo[d]imidazole derivatives of piperidine and piperazine are 5-piperazinyl and 5-piperadinyl-1H-benzo[d]imidazol-2(3H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a selected biaryl group, or a pharmaceutically acceptable salt thereof. The piperidinyl compounds are prepared by removal of the Boc group from tert-Butyl-4-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carboxylate. Subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The piperazinyl compounds are prepared by preparation of the intermediate tert-Butyl 4-(3,4-diaminophenyl)piperazine-1-carboxylate. Removal of the Boc group and subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.

专利号:US-9073900-B2
优先权日:2013-10-02
标题:Dihydroquinone derivatives of piperidine and piperazine
发明人：ULLAH NISAR
权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH
摘要:The dihydroquinone derivatives of piperidine and piperazine are 7-piperazinyl and 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a group selected from a through f having the formula:n n nor a pharmaceutically acceptable salt thereof. The piperazine compounds are prepared by condensing 4-bromo-2-nitro-benzonitrile with 1-Boc-piperazine (1-tert-butoxycarbonyl-piperazine) to form an intermediate that is converted to a piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones. The piperadinyl compounds are prepared from tert-butyl-4-(2-oxo-1,2,3,4-tetradihydroquinazolin-7-yl)piperidine-1-carboxylate, which is converted to 7-(piperidin-4-yl)-3,4-dihyroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones.

专利号:US-2024309013-A1
优先权日:2021-11-19
标 题:SYNTHESIS OF 2'-(7,7-dimethyl-1'H,7H-spiro[furo[3,4-b]pyridine-5,4'-piperidin]-1'-yl)-1,3-dihydro-4'H-spiro[indene-2,5'-[1,3]oxazol]-4'-one
发明人：ADAM JEAN-MICHEL; BACHMANN STEPHAN; BIGLER RAPHAEL; DOTT PASCAL; FANTASIA SERENA MARIA; GROSSE-SENDER KATJA; JAMES PHILIPPE; SPURR PAUL; THUN JUERGEN; TONAZZI SANDRO; TOSATTI PAOLO
权利人:HOFFMANN LA ROCHE
摘要:The invention provides crystalline forms of 2′-(7,7-dimethyl-1′H,7H-spiro[furo[3,4-b]pyridine-5,4′-piperidin]-1′-yl)-1,3-dihydro-4′H-spiro[indene-2,5′-[1,3]oxazol]-4′-one, and a process for converting Form A to Form B for use in medicaments for treatment of anxiety, depression, irritability, impaired social interactions and psychomotor coordination, and other indications. The invention further provides processes to manufacture 2′-(7,7-dimethyl-1′H,7H-spiro[furo[3,4-b]pyridine-5,4′-piperidin]-1′-yl)-1,3-dihydro-4′H-spiro[indene-2,5′-[1,3]oxazol]-4′-one. Also disclosed are compounds useful as intermediates in the methods of the invention.

专利号:WO-2004058727-A1
优先权日:2002-12-20
标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
发明人：CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

专利号:US-2022363662-A1
优先权日:2021-04-20
标题 :Compounds as lxr agonists
发明人：PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V
权利人:INTEGRAL BIOSCIENCES PRIVATED LTD
摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: