Synthesis of biologically compounds to control of the signal transduction by an application of phophorus functional group
Synthesis of biologically compounds to control of the signal transduction by an application of phophorus functional group
批准号:
12672067
负责人:
SHIBUYA Shiroshi
金额:
$1.79万
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (C)
财政年份:
2000
资助国家:
日本
项目状态:
已结题
起止时间:
2000 至 2001
中文摘要
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英文摘要
A variety of biologically active compounds to control of the signal transduction were synthesized. The results can be classified into following items1.A variety of nucleotide analogues having a were cynthesized by condensation of cyclic and acyclic alkyl spacer containing difluoromethylenephosphonic acid moiety were synthesized and condensed with nucleic acid base to get high inhibitory activity to purine nucleoside phosphorylase.2.Sphingomyelin analogous compounds containing difluoromethylenephosphonic acid moiety were synthesized starting with L-serine and D-serine for the evaluation of their inhibitory potency to sphingomyelinase.3.Cyclopropyl carbinols possessing a difluoromethylenephosphonate group were synthesized by reduction of the corresponding ketones.4.Cyclohexane derivative possessing a (diethoxyphosphinyl)difluoromethyl unit were synthesized by the Diels-Alder rection of the 1, 3-butadinene possessing a (diethoxyphosphinyl)difluoromethyl group with dienophiles.5.β-Amino acid derivatives possessing a nucleic acid base were prepared by an application of kinetic resolution of 3-subsituted 1, 3-propane diol as the key reaction.6.Diastereoselective synthesis of chiral β-amino-α-hydroxy-H-phosphinates by hydrophosphinylation of a-amino acids in the prsence of chiral catalyst.
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Tsutomu Yokomatsu: "1, 3-Dipolar Cycloadition of Diazomethane to, 1, 1-Difluoro-allylphosphonates : Application to Synthesis of Cyclo Propane Derivatives Having a Diethoxyphosphoryldifluoromethylene Unit"Heterocycles. 56. 273-282 (2002)
Tsutomu Yokomatsu:“重氮甲烷到 1, 1-二氟-烯丙基膦酸酯的 1, 3-偶极环加成:在合成具有二乙氧基磷酰基二氟亚甲基单元的环丙烷衍生物中的应用”杂环。
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Takehiro Yamagishi: "Diastereoselective Synthesis of Chifal β-Amino-αhydroxy-H-phosphinates though Hydrophos phinylation of α-Amino Aldehydes"Tetrahedron Lett.. Vol.42. 5033-5036 (2001)
Takehiro Yamagishi:“通过 α-氨基醛的氢膦酰化非对映选择性合成 Chifal β-氨基-α羟基-H-次膦酸盐”Tetrahedron Lett.. Vol.42 (2001)。
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Tsutomu Yokomatsu: "Synthesis of Aryldifluoromethylphosphothioic Acid from O,O-Diethyl Aryldifluoromethylphosphosphonothioates"J.Organic Chemistry. 65. 5858-5861 (2000)
Tsutomu Yokomatsu:“从O,O-二乙基芳基二氟甲基硫代磷酸酯合成芳基二氟甲基硫代磷酸”J.有机化学。
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Tsutomu Yokomatsu: "Synthesis of allenic (α,α-Difluoromethylene) phosphosnates from Propar gylic Tosylates and Acetates Synthesis of allenic (α,α-Difluoromethylene )phosphonates from Propargylic Tosylates and Acetates"Synlett. 287-289 (2000)
Tsutomu Yokomatsu:“从甲苯磺酸丙炔酯和乙酸酯合成联二烯(α,α-二氟亚甲基)磷酸酯从甲苯磺酸丙炔酯和乙酸酯合成联烯(α,α-二氟亚甲基)膦酸酯”Synlett 287-289(2000)。
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Tsutomu Yokomatsu: "Diels-Alder Cycloadition of Novel Buta-1,3-dieneDerivatives Prossessing a (Diethoxy-phosphinoyl)-difluoronethyl Unite"Chemical Commun.. 1878-1879 (2001)
Tsutomu Yokomatsu:“新型 Buta-1,3-diene 衍生物的 Diels-Alder 环化反应生成(二乙氧基膦酰基)-二氟乙基单元”Chemical Commun. 1878-1879 (2001)
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共 24 条
synthesis of biologically active compounds for the conrol of signal transduction by using phosphorus functional group
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批准号:09672162
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项目类别:Grant-in-Aid for Scientific Research (C)
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资助金额:$1.98万
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财政年份:1997
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负责人:SHIBUYA Shiroshi
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依托单位: