专利号:US-4739073-A 优先权日:1983-11-04 标题:Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof 发明人:KATHAWALA FAIZULLA G 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein one of R and Ro is and the other is primary or secondary C1-6alkyl not containing an asymmetric carbon atom, C3-6cycloalkyl or phenyl(CH2)m-, wherein R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy, and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C3-6cycloalkyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH-, wherein n is 0, 1, 2 or 3, and Z is wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, benzyl or M, wherein M is a pharmaceutically acceptable cation, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level, and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:US-6875866-B2 优先权日:2002-02-21 标题:Process for synthesis of D1 receptor antagonists 发明人:DAHANUKAR VILAS H; ECKERT JEFFREY M; GALA DINESH; LUCAS BRIAN; SCHUMACHER DORIS P; ZAVIALOV ILIA 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of a compound of formula n n nand intermediates therefor.
专利号:US-9802934-B2 优先权日:2013-10-17 标 题 :Process for the synthesis of (R)-praziquantel 发明人:QIAN MINGXIN 权利人:TONGLI BIOMEDICAL CO LTD 摘要:The present disclosure relates to a process and new intermediates for the synthesis of (R)-praziquantel, which is obtained through four steps in proper order, that is, condensation reaction, reduction reaction, acylation reaction and ring-closing reaction, using (1R)-2-substituted-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid as starting material. Overall, the present disclosure provides a (R)-praziquantel product with higher optical purity through a process route that is more cost effective and environmentally friendly.
专利号:US-7189849-B2 优先权日:1997-02-10 标 题:Synthesis of acyclic nucleoside derivatives 发明人:LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY 权利人:MEDIVIR AB 摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.
专利号:US-2013133483-A1 优先权日:2010-03-08 标题 :Synthesis of Nanoparticles Using Reducing Gases 发明人:YANG HONG; WU JIANBO; SHI MIAO; GROSS ADAM 权利人:YANG HONG; WU JIANBO; SHI MIAO; GROSS ADAM; UNIV ROCHESTER 摘要:Selective gas-reducing methods for making shape-defined metal-based nanoparticles. By avoiding the use of solid or liquid reducing reagents, the gas reducing reagent can be used to make shape well-defined metal- and metal alloy-based nanoparticles without producing contaminates in solution. Therefore, the post-synthesis process including surface treatment become simple or unnecessary. Weak capping reagents can be used for preventing nanoparticles from aggregation, which makes the further removing the capping reagents easier. The selective gas-reducing technique represents a new concept for shape control of nanoparticles, which is based on the concepts of tuning the reducing rate of the different facets. This technique can be used to produce morphology-controlled nanoparticles from nanometer- to submicron- to micron-sized scale. The Pt-based nanoparticles show improved catalytic properties (e.g., activity and durability).
专利号:US-2006241298-A1 优先权日:2005-04-21 标 题:Methods for synthesis of dicarbamate compounds and intermediates in the formation thereof 发明人:MORTKO HENRY; HE WEIXUAN; ANDERSEN MARC W; DOTSE ANTHONY K; LI JIE 权利人:MORTKO HENRY; HE WEIXUAN; ANDERSEN MARC W; DOTSE ANTHONY K; LI JIE 摘要:Disclosed is a method of making 2-substituted-2-halo-1,3-propanediols via reduction of corresponding malonate compounds. Also disclosed is a method of making 2-substituted-2-halo-1,3-dicarbamate compounds (such as halo derivatives of felbamate, including fluorofelbamate) via reduction of malonate compounds, followed by carbamoylation. Reduction of the malonate compounds is carried out using an electrophilic hydride reagent.