📜香草醛置于盐酸,一氯化碘体系中,化学反应 73.0H,以80%的收率获得产物5-碘香兰素 参考文献:Design,Synthesis And Cytotoxic Activity Evaluation Of New Aminosubstituted Benzofurans 标题:Design,Synthesis And Cytotoxic Activity Evaluation Of New Aminosubstituted Benzofurans 摘要:我们制备了一些新的氨基取代苯并呋喃类似物,并研究了它们对五种人类肿瘤细胞系(mcf-7,Skbr3,Skov3,Hct-116 和 Hela)的细胞毒性/细胞抑制活性.某些化合物显示出明显的肿瘤细胞生长抑制作用,表明可能存在结构-活性关系. DOI:10.2174/15734064113096660049
专利号:US-5175302-A 优先权日:1987-07-13 标 题 :Nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4837327-A 优先权日:1987-07-13 标 题 :Process for nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4999429-A 优先权日:1989-01-09 标 题 :Process for the preparation of α,α,β-1-trifluoro-1-olefinic derivatives 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-7507851-B2 优先权日:2003-09-24 标 题 :Halocombstatins and methods of synthesis thereof 发明人:PETTIT GEORGE R; MINARDI MATHEW D; ROSENBERG HEIDI J 权利人:ARIZONA BOARD OF REGENTS A STA 摘要:The invention relates to novel compounds denominated halocombstatins. The halocombstatins are derivatives of combretastatin A-3, and include compounds that exhibit cancer growth cell inhibition against a panel of human cancer cell lines and the murine P388 leukemia, as well as activity as inhibitors of tubulin polymerization and inhibitors of the binding of colchicine to tubulin.
专利号:US-6403814-B1 优先权日:1998-10-16 标 题 :Method for synthesizing diaryl-substituted heterocyclic compounds, including tetrahydrofurans 发明人:RAO ALLA VENKATA RAMA; CHORGHADE MUKUND S; ISLAM AMIN UL; RAO VEMURI VENKATA KIRAN; PRASAD ANEGONDI SREENIVASA; RAO BATCHU VENKATESWARA; REDDY RANGA; REDDY LALATA KRISHNAKANTH; SHAILAJA KOTAKONDA; GURJAR MUKUND KESHAO; MHASKAR SUNIL VYANKATESH 权利人:MILLENNIUM PHARM INC 摘要:A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (±)trans-2-[5-N'-methyl-N'-hydroxyureidyl-methyl)3-methoxy-4-p-chlorophenylthioethoxyphenyl]-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.
专利号:US-2002128491-A1 优先权日:1999-10-15 标题 :Method for synthesizing diaryl-substituted heterocyclic compounds, including tetrahydrofurans 发明人:RAO ALLA VENKATA RAMA; CHORGHADE MUKUND S; ISLAM AMIN UL; RAO VEMURI VENKATA KIRAN; PRASAD ANEGONDI SREENIVASA; RAO BATCHU VENKATESWARA; REDDY RANGA; REDDY LALATA KRISHNAKANTH; SHAILAJA KOTAKONDA; GURJAR MUKUND KESHAO; MHASKAR SUNIL VYANKATESH 摘要:A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (±) trans-2-[5-(N′-methyl-N′-hydroxyureidyl-methyl)-3-methoxy-4-p-chlorophenylthioethoxyphenyl]-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.