A Facile Method for the N-Alkylation of N-Boc-aminothiophenes

A Facile Method for the N-Alkylation of N-Boc-aminothiophenes

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摘要　　2-( N-Alkylamino)thiophene and its derivatives are the key intermediates for the synthesis of quinazoline-basedthymidylate synthase inhibitors containing thiophene ring such as Raltitrexed, [1] which has been used widely for thefirst-line treatment of advanced colorectal cancer. [2]……

作者 CAO Sheng-Li FENG Yu-Ping WAN Rong

机构地区 Department of Chemistry

出处《有机化学》 SCIE CAS CSCD 北大核心 2003年第z1期219-219,共1页 Chinese Journal of Organic Chemistry

基金 Project supported by the Natural Science Foundation of Beijing City, the Education Committee of Beijing City and the Ministry of Education of Chi na.

分类号 O62 [理学—有机化学]

作者简介 CAO Sheng-Li E-mail: caoshengli @ tsinghua. org. cn

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1[1]Marsham, P. R.; Hughes, L. R.; Jackman, A. L.; Hayter, A. J.; Oldfield, J.; Wardleworth, J. M.; Bishop, J. A. M.; O'Connor, B. M.; Calvert, A. H. J. Med. Chem. 1991, 34, 1594.
2[2]Cunningham, D.; Zalcberg, J.; Maroun, J.; James, R.; Clarke, S.; Maughan, T. S.; Vincent, M.; Schulz, J.; Baron, M. G.; Facchini, T. Eur. J. Cancer 2002, 38, 478.

1CAO Sheng-Li WAN Rong FENG Yu-Ping.A New Route for the Synthesis of Thymidylate Synthase Inhibitor Raltitrexed[J].有机化学,2003,23(z1):220-220. 被引量：1
2A Facile Method for the Synthesis of N-trifluoroacetyl-α, β-daunosamine[J].厦门大学学报（自然科学版）,1999,38(S1):21-21.
3赵华绒,俞庆森.A General Two-Step Procedure for the N-Alkylation of Seleno-amides[J].Chinese Journal of Chemistry,2002,20(9):891-894. 被引量：2
4Xue Gong SHE,Wen Xin GU,Hua WANG,Xin Fu PAN(Department of Chemistry,National Laboratory of Applied Oerganic Chemistry，Lanzhou University,Lanzhou 730000).Stereoselective Synthesis of 2-(4-Hydroxyphenyl)-3-hydroxymethyl-1,4-benzodioxane-6-aldehyde—The Key Intermediate of Sinaiticin[J].Chinese Chemical Letters,1999,10(2):107-108.
5赵惠明,张洋,陈洁.Vibrational Spectroscopic Study of (E)-3-(4-fluorophenyl)-N-[4-(phenylamino) quinazoline-7-yl] Acrylamide[J].Chinese Journal of Structural Chemistry,2012,31(8):1111-1120.
6CAO Sheng-Li FENG Yu-Ping WAN Rong LI Run-Tao.Synthesis of Dithiocarbamate Derivatives of Quinazolinone and Their in vitro Antitumor Activity[J].有机化学,2003,23(z1):221-221.
7Aida Chaker,Fathi Zribi,Franoise Nepveu,Fakher Chabchoub.Microwave irradiation: Novel and facile methods for the synthesis of new pyrimidinones[J].Chinese Chemical Letters,2014,25(8):1207-1210.
8Ya-Qiong Li,Yun-Bin Chen,Zhi-Zhen Huang.Direct N-alkylation of amines with alcohols using AlCl_3 as a Lewis acid[J].Chinese Chemical Letters,2014,25(12):1540-1544. 被引量：2
9Zheng, QY,Chen, CF,Huang, ZT.A Facile Method to Synthesize Spiro-calix[4]arenes[J].Chinese Chemical Letters,2000,11(10):863-864.
10De Ling Zhou Ye Di Guan Sheng Jin Department of Chemistry,Peking University,Beijing,100871.A NEW ONE-STEP REDUCTIVE N-ALKYLATION OF AMINO ACIDS AND THEIR ESTERS[J].Chinese Chemical Letters,1990,1(3):209-210.

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A Facile Method for the N-Alkylation of N-Boc-aminothiophenes

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