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丁酸,氯甲酸异丁酯 以 四氢呋喃,N-甲基吡咯烷酮 作为反应溶剂,化学反应 0.5H,反应生成 丁酸异丁酯
参考文献:溶血素e的十四种衍生物的全合成和功能评价:阳离子,疏水和芳香部分对抗菌活性的重要性.
标题:溶血素e的十四种衍生物的全合成和功能评价:阳离子,疏水和芳香部分对抗菌活性的重要性.
摘要:溶血素e(1)是结构复杂的37元十肽,包含12个氨基酸残基,具有n-甲基化酰胺和酯键.化合物1与细菌膜中的甲萘醌(mk)结合,发挥其强大的杀菌活性.破译内这种独特的抗生素的生物学上重要的功能性,我们通过系统地改变侧链结构进行一个全面的结构-活性关系(sar)研究升-Thr-1,ð-Arg-2,N-Me-D-Phe-5,D-Arg-7,L-Glu-8和d-Trp-10.首先,我们实现的14个新的侧链类似物的全合成1通过采用固相策略.然后,我们通过1及其类似物评估了mk依赖的脂质体破坏和对金黄色葡萄球菌的抗菌活性.脂质体和细菌实验之间的相关数据表明,膜裂解主要是抗菌功能的原因.将d-Arg-2-7的阳离子胍基改变为中性酰胺,将l-Thr-1的c7-酰基取代为c2或c11对应物,其抗菌活性降低了4倍或8倍.更剧烈地是d ‐trp‐10到d的化学突变‐ala‐10完全废除了
DOI:10.1002/chem.201604022

专利信息

专利号:US-3887490-A
优先权日:1970-08-27
标 题 :Process for regenerating noble metal catalyst for the synthesis of hydrogen peroxide according to the anthraquinone process
发明人：SCHREYER GERD; THEISSEN FERDINAND; WEIBERG OTTO; WEIGERT WOLFGANG
权利人:DEGUSSA
摘要:In situ regeneration of noble metal catalysts for the synthesis of hydrogen peroxide by the anthraquinone process is provided by employing as the working solution coming from the extraction or desorption step and being introduced into the hydrogenation step a solution which contains at least 250 mg/liter of hydrogen peroxide, to thereby completely regenerate the noble metal catalyst by full capacity of the hydrogenation step.

专利号:US-6835841-B2
优先权日:2002-09-13
标 题:Asymmetric catalytic hydrogenation process for preparation of chiral cyclic β-aminoesters
发明人：DEERBERG JOERG; MCLEOD DOUGLAS D; YUE TAI-YUEN
权利人:BRISTOL MYERS SQUIBB CO
摘要:A novel process for the asymmetric synthesis of substituted cyclic beta-amino-carboxylates of the type shown in the specification from appropriate beta-enamino-ester starting materials is described. These compounds are useful as intermediates for MMP and TACE inhibitors.

专利号:EP-0946499-B1
优先权日:1996-11-22
标 题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK NORMAN; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R<1> is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R<2> is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R<3> and R<3'> are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R<7>)n(W)p, wherein R<7> is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH( phi )CH2C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R<1> to -CX'X''-, oxygen and sulfur.

专利号:EP-0951464-B1
优先权日:1996-11-22
标题:N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; THORSETT EUGENE D; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; JOHN VARGHESE; FANG LAWRENCE Y; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:EP-0951466-B1
优先权日:1996-12-23
标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6262302-B1
优先权日:1996-11-22
标题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK N; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.