3-氯苯乙烯 反应生成 吲哚啉 参考文献:Process For The Preparation Of 2,3-Dihydroindoles (Indolines),Novel 2,3-Dihydroindoles,And Their Use 标题:Process For The Preparation Of 2,3-Dihydroindoles (Indolines),Novel 2,3-Dihydroindoles,And Their Use 摘要:一种制备式为(I)的2,3-二氢吲哚的方法,通过式为(Iia)或(Iib)的卤代苯乙烯与式为(Iii)R1-nh2的胺在至少一种惰性溶剂或水中反应,并在至少一种碱存在下进行.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2024092821-A1 优先权日:2020-03-31 标题:Synthesis of oligonucleotides and related compounds 发明人:ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA 权利人:JANSSEN BIOPHARMA INC 摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.
专利号:US-4902817-A 优先权日:1987-09-17 标 题 :Process for the synthesis of alpha n alkylated amino acids and esters thereof, application to the synthesis of carboxyalkyl dipeptides 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R 1 is linear or branched lower alkyl with 1 to 6 carbon atoms, n R 2 is a linear or branched lower alkyl with 1 to 4 carbon atoms, n employing inexpensive starting materials and obtaining optimum yields. n Application to the synthesis of carboxyalkyl dipeptides.
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
专利号:US-11542269-B2 优先权日:2018-01-03 标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHOI HYEONG-WOOK; FANG FRANCIS G 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
参考文献:10.2147/cia.s13803 摘要:Yoshida M, Kudoh J, Homma Y, Kawabe K. Safety and efficacy of silodosin for the treatment of benign prostatic hyperplasia. Clin Interv Aging. 2011;6():161–72. 参考文献:10.1107/s160053681100691x 摘要:Qiao Z, Liu L, Wang D. tert-Butyl 3-benzyl-3-[(E)-2-benzyl-idene-3-oxocyclo-pent-yl]-2-oxoindoline-1-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o858. 参考文献:10.1107/s1600536811008890 摘要:Gainsford GJ, Ashraf M, Kay AJ. 2-{[(Biphenyl-2-yl)diazen-yl]methyl-idene}-1,3,3-trimethyl-indoline. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o893. 参考文献:10.1107/s1600536811014590 摘要:Gainsford GJ, Ashraf M, Kay AJ. 4-tert-Butyl-2-[2-(1,3,3-trimethyl-indolin-2-yl-idene)ethyl-idene]cyclo-hexa-none. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1210. 参考文献:10.1107/s1600536811019143 摘要:Lin N, Chen MM, Deng YQ, Luo RS, Ng SW. (S)-2-(1-Methyl-indolin-2-yl)-1,3-diphenyl-propan-2-ol. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1515.