CAS: 6305-38-0; 3-Aminodihydrofuran-2(3H)-One Hydrobromide

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42417-39-0 104347-13-9 2185-03-7

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L-methionine bromoacetic acid (S)-methioninol DL-Homoserine 1-(2-oxo-tetrahydrofuran-3-yl)-3-phenylurea N-phenylthi°Carbamoyl-DL-homoserine lactoneN-phenylthi°Carbamoyl-DL-homoserine lactone (S)-3-(N-benzyloxycarbonylamino)tetrahydrofuran-2-one N-butyryl-DL-homoserine lactone

Dl-高丝氨酸置于氢溴酸体系中,化学反应 3.0H,以81%的收率获得产物α-氨基-γ-丁内酯氢溴酸盐
参考文献:Cyclic Hydroxamates,Especially Multiply Substituted [1,2]Oxazinan-3-Ones
标题:Cyclic Hydroxamates,Especially Multiply Substituted [1,2]Oxazinan-3-Ones
摘要:报道了将假定的n-酰-D-阿拉-D-阿拉替代物的合成途径,从将4,5和6元环内酯转化为5,6和7元环氢氧化物开始.合成的关键步骤是ω-氨氧酯的三甲基铝促进的环化反应.7元环氢氧化物以椅式构象结晶.将反应序列扩展到同型丝氨酸或同型丝氨酸内酯会导致环康纳林和n-酰化环康纳林的形成.环康纳林的4-苯乙酰氨基衍生物以船式构象结晶.在环康纳林的4-酰氨基环康纳林的环氮上附加2-羧基丙基取代基,可以通过将无环氨氧酯前体与苄乳酸三甲酯的三氟甲磺酸酯偶联,或在环化之后,通过与三氟甲基丙酸叔丁酯在氟化钾-氧化铝存在下偶联,然后在每种情况下去除保护基来实现.通过4-苯乙酰氨基环康纳林与苄基2-氧戊二酸酯在异亚胺存在下反应,然后进行氢解,合成了抗生素拉维西汀的六元同系物.从甲基2,4-二溴-2,4-二去氧-L-赤葡萄糖酸甲酯开始,该物质可以从抗坏血酸中经过两步合成,这些反应序列已被应用于立体特异性合成一种d-丙氨酸衍生物,其氮原子被包含在一个3,4-二取代[1,2]噁唑烷-3-酮内.关键词:D-Ala-D-Ala替代物,环康纳林,同型拉维西汀,肽聚糖,三甲基铝.
DOI:10.1139/v03-122

专利信息

专利号:US-7390801-B2
优先权日:1996-12-23
标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J
权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI
摘要:Disclosed are compounds 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-11434242-B2
优先权日:2017-12-04
标题:Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO ERNO; BELIAEV ALEXANDER; ROSSI TINO; PALMA PEDRO NUNO LEAL; SOARES DA SILVA PATRÃ?CIO MANUEL VIEIRA ARAUJO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & Cª S A; BIAL—PORTELA & CA S A
摘要:This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-2003232820-A1
优先权日:2001-08-29
标题:Method for synthesizing oxazinones
发明人：WOLFE SAUL; WILSON MARIE-CLAIRE; CHENG MING-HUEI
摘要:New methods and intermediates are discussed for the stereospecific synthesis of oxazinone compounds.

专利号:EA-002100-B1
优先权日:1996-12-23
标题:CYCLOALCYL COMPOUNDS, LACTAMS, LACTONES AND RELATED COMPOUNDS CONTAINING THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING THE SURVIVAL AND / OR SYNTHESIS OF β-AMYLOUS PEPTIDE SOFTWARE AGREED SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE AND SOFTWORK

专利号:CN-103524464-A
优先权日:2013-10-24
标 题 :Synthesis of Immune Haptens of AHL-like Signaling Molecules in Phytopathogenic Bacteria

专利号:US-2002045747-A1
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