专利号:EP-1108724-B1 优先权日:1996-01-16 标题 :Synthesis of methoxy nucleosides and enzymatic nucleic acid molecules 发明人:WINCOTT FRANCINE; BEIGELMANN LEONID; MATULIC-ADAMIC JASENKA; USMAN NASSIM; HAEBERLI PETER; KARPEISKY ALEXANDER; SWEEDLER DAVID; JARVIS THALE; DIRENZO ANTHONY 权利人:SIRNA THERAPEUTICS INC 摘要:This invention relates to chemical synthesis of 2'-O-methyl, 3'-O-methyl and 5'-O-methyl nucleosides, incorporation of novel chemical modifications in enzymatic nucleic acid molecules and improved methods for the synthesis of enzymatic nucleic acid molecules.
专利号:US-4310467-A 优先权日:1980-10-22 标题:Process and intermediates for the synthesis of vitamin D3 metabolites 发明人:BATCHO ANDREW D; BERGER JR DONALD E; USKOKOVIC MILAN R 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D 3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D 3 metabolites.
专利号:US-6972330-B2 优先权日:1996-02-13 标题:Chemical synthesis of methoxy nucleosides 发明人:BEIGELMAN LEONID; HAEBERLI PETER; KARPEISKY ALEXANDER; SWEEDLER DAVID 权利人:SIRNA THERAPEUTICS INC 摘要:Process for chemical synthesis of methoxy nucleosides.
专利号:US-11976081-B2 优先权日:2019-04-26 标题 :Intermediate of eribulin and synthesis method and use thereof 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.
专利号:US-9284336-B1 优先权日:2014-08-21 标题 :Synthesis of 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate and analogs 发明人:LAALI KENNETH K 权利人:LAALI KENNETH K; UNIV NORTH FLORIDA 摘要:4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate salt was synthesized and isolated. The pentafluorosulfanyl salt was examined in a wide assortment of reactions to form novel SF 5 -bearing alkenes, alkynes, and biaryl derivatives using Heck-Matsuda, Sonogashira, and Suzuki coupling protocols. Dediazoniation of the salt furnished the corresponding p-SF 5 —C 6 H 4 X, C 6 H 4 OS(O)(CF 3 )â•?NSO 2 CF 3 , and p-SF 5 —C 6 H 4 —NTf 2 derivatives. The azide derivative p-SF 5 —C 6 H 4 N 3 entered into click chemistry with phenylacetylenes to furnish the corresponding triazoles. Various SF 5 -bearing alkenes were synthesized by coupling reactions using a metal catalyst. Fluorodediazoniation selectively furnished the fluoro derivative p-SF 5 —C 6 H 4 F. Homolytic dediazoniation gave the unsymmetrical biaryls, thus demonstrating the broad utility of pentafluorosulfanyl diazonium salts as building blocks of SF5-aromatics that are in high demand in many branches of chemistry including biomedicine and materials chemistry.
专利号:US-5866335-A 优先权日:1994-06-24 标题:Preparation of derivatized 10,10'-substituted-9,9'-biacridine luminescent molecules and signal solutions 发明人:KATSILOMETES GEORGE W; HO PAK T 权利人:KATSILOMETES GEORGE W 摘要:The synthesis of 10,10'-substituted-9,9'-biacridine molecules and their derivatives is disclosed. These molecules are shown to catalyze the production of light by chemiluminescence in the presence of a signal solution having at a pH from about 10.0 to about 14.0, at a concentration effective for producing a chemiluminescent signal, a chelating agent, a sulfoxide, a reducing sugar, an oxidant or combination of oxidants, an alcohol and aqueous sodium tetraborate. These 10,10'-substituted-9,9'-biacridines are used alone or attached to haptens or macromolecules and are utilized as labels in the preparation of chemiluminescent, homogeneous or heterogeneous assays. They are also used in conjunction with other chemiluminescent label molecules to produce multiple analyte chemiluminescent assays.
摘要:McKenna, C. E.; Kashemirov, B. A.; Błażewska, K. M., Science of Synthesis, (2009) 42, 900. 参考文献:10.1007/bf01192866 摘要:Murkovic M, Hillebrand A, Winkler J, Leitner E, Pfannhauser W. Variability of fatty acid content in pumpkin seeds (Cucurbita pepo L.). Z Lebensm Unters Forsch. 1996 Sep;203(3):216–9. doi: 10.1007/bf01192866. 参考文献:10.1007/bf01088494 摘要:Barampama Z, Simard RE. Effects of soaking, cooking and fermentation on composition, in-vitro starch digestibility and nutritive value of common beans. Plant Foods Hum Nutr. 1995 Dec;48(4):349–65. doi: 10.1007/bf01088494. 参考文献:10.1007/bf00114621 摘要:Amund OO. Utilization and degradation of an ester-based synthetic lubricant by Acinetobacter lwoffi. Biodegradation. 1996 Apr;7(2):91–5. doi: 10.1007/bf00114621. 参考文献:10.1007/bf02562302 摘要:Borod E, Atkinson R, Barclay WR, Carlson SE. Effects of third trimester consumption of eggs high in docosahexaenoic acid on docosahexaenoic acid status and pregnancy. Lipids. 1999;34 Suppl():S231. doi: 10.1007/bf02562302.