CAS: 102089-74-7; Boc-D-Phenylglycinol

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117049-14-6 67341-01-9 20989-17-7

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styrene N-chloro-N-sodio-tert-butylcarbamate tert-butyl dicarbonatedi-tert-butyl dicarbonate 2-azido-2-phenylethanol D-2-phenylglycinol (2S)-2-phenylglycinol tert-butyl ester[2-(isoquinolin-7-yloxy)-1-phenyl-ethyl]-carbamic acid tert-butyl ester 4-phenyl-2-oxazolidinone

左旋苯甘氨酸置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应生成Boc-D-苯甘氨醇
参考文献:具有较长手性取代基的烟碱乙酰胆碱受体和硝基亚甲基新烟碱衍生物的对接模型及其生物学活性
标题:具有较长手性取代基的烟碱乙酰胆碱受体和硝基亚甲基新烟碱衍生物的对接模型及其生物学活性
摘要:在本研究中,合成具有在咪唑烷环上第5位含有硫原子,氧原子或芳香环的取代基的硝基亚甲基新烟碱衍生物,以评估其对烟碱乙酰胆碱受体(nachr)的亲和力及其对成年雌性家蝇的杀虫活性. .将烷基化衍生物的受体亲和力与具有醚或硫醚基团的化合物的受体亲和力进行比较后发现,碳原子向硫原子的转化不会影响受体亲和力,而向氧原子的转化则对受体亲和力不利. .具有苄基或苯基的化合物的受体亲和力低于未取代的化合物.连接在咪唑烷环上第5位的正丁基.对nachr-配体模型的对接研究表明,通过掠过形成结合区的氨基酸,配体结合区会随着取代基长度的增加而扩展.通过考虑log P和取代基中杂原子(包括硫和氧原子)的数量,化合物的杀虫活性与受体亲和力呈正相关,这表明杀虫活性受受体亲和力,疏水性和代谢稳定性的影响的化合物.
Doi:10.1016/j.Bmc.2014.12.058

专利信息

专利号:US-11858901-B2
优先权日:2019-10-30
标 题:3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6 trifluoromethyl benzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, process for its preparation, and its use in the synthesis of elagolix
发明人：BALLETTE ROBERTO; JIMÉNEZ ALONSO OSCAR; GARCÃ?A GARCÃ?A ELENA; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-11840519-B2
优先权日:2019-09-03
标 题 :Process for the synthesis of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2.6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process
发明人：LENNA ROBERTO; FASANA ANDREA; ORTIZ JERRY
权利人:IND CHIMICA SRL
摘要:The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:

专利号:US-2022411382-A1
优先权日:2019-10-30
标 题 :3-((r)-2-(amino-2-phenylethyl)-1-(2-fluoro-6 trifluoromethyl benzyl)-5-iodo-6-methyl-1h-pyrimidine-2,4-dione or a salt thereof, process for its preparation, and its use in the synthesis of elagolix