Novel applications of resin bound #alpha#-amino acids for the synthesis of benzodiazepines (via Wang resin) and ketopiperazines(via hydroxymethyl resin)

Hulme Chistopher; Ma Liang; Kumar Vasant

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Novel applications of resin bound #alpha#-amino acids for the synthesis of benzodiazepines (via Wang resin) and ketopiperazines(via hydroxymethyl resin)

机译：树脂结合的＃α＃-氨基酸在苯并二氮杂卓（通过Wang树脂）和酮哌嗪（通过羟甲基树脂）的合成中的新应用

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This communication reveals a novel application of resin bound #alpha#-amino acids coupled with the UDC (Ugi/DeBOC/cyclize)strategy.Reation with either N-BOC-#alpha#-amino aldehydes or N-BOC anthranilic acids and subsequent acid treatment allows the preparation of highly pure and diverse arrays (approx.10000 in size)of 1,4-benzodiazepines (Wang resin) and ketopiperazines (hydroxymethyl resin),respectively.Notable for the benzodiazepine series of compounds are the five potential points of diversity available from this two-step protocol.

机译：这种交流揭示了树脂结合的＃alpha＃-氨基酸与UDC（Ugi / DeBOC / cyclize）策略的新应用。与N-BOC-＃alpha＃-氨基醛或N-BOC邻氨基苯甲酸和随后的酸反应通过处理，可以分别制备1,4-苯并二氮杂pine（Wang树脂）和ketopiperazines（羟甲基树脂）的高纯度和多样化的阵列（值得注意的是）。苯并二氮杂series系列化合物值得注意的是五个潜在的多样性点可从此两步协议中获得。

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《Tetrahedron letters: The International Journal for the Rapid Publication of Preliminary Communications in Organic Chemistry》 |2000年第10期|共6页
作者
Hulme Chistopher; Ma Liang; Kumar Vasant;
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正文语种 eng
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1. Novel applications of resin bound #alpha#-amino acids for the synthesis of benzodiazepines (via Wang resin) and ketopiperazines(via hydroxymethyl resin) [J] . Hulme Chistopher, Ma Liang, Kumar Vasant Tetrahedron letters: The International Journal for the Rapid Publication of Preliminary Communications in Organic Chemistry . 2000,第10期

机译：树脂结合的＃α＃-氨基酸在苯并二氮杂卓（通过Wang树脂）和酮哌嗪（通过羟甲基树脂）的合成中的新应用
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机译：磺酸官能化的王树脂（Wang-OSO3H）作为聚合酸性催化剂，可用于环保合成2,3-二氢喹唑啉-4（1H）-ones
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6. Distributed Drug Discovery Part 2: Global Rehearsal of Alkylating Agents for the Synthesis of Resin-Bound Unnatural Amino Acids and Virtual D3 Catalog Construction [O] . William L. Scott, *, Jordi Alsina, -1

机译：分布式药物发现第2部分：用于树脂结合的非天然氨基酸合成的烷基化剂的全球演练和虚拟D3目录构建
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8. Application of Optical Methods, Including Optical Interference, to Measure the Dimensional Stability of Resins, Resin Based Adhesives and Resin Based Composites [R] . Ashbee, K. H. G., Sargent, J. P. 1983

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Novel applications of resin bound #alpha#-amino acids for the synthesis of benzodiazepines (via Wang resin) and ketopiperazines(via hydroxymethyl resin)

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