专利号:US-7956011-B2 优先权日:2005-05-04 标题:Materials and methods for the photodirected synthesis of oligonucleotide arrays 发明人:SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN 权利人:CANCER RES INST ROYAL 摘要:Materials and methods for photodirected synthesis of oligonucleotide arrays on a solid substrate by photodirected synthesis are disclosed which employ a film formed from (i) a photoacid generator that on photolysis generates acid that is capable of directly removing the protecting group of the linker molecules or oligonucleotides and (ii) a polymer substantially lacking electronegative heteroatoms that are capable of hydrogen bonding with photogenerated acid. Methods of synthesizing an oligomer arrays are also described that use a film that restricts diffusion of reactants and products on the substrate during synthesis of the array and which includes a precursor of a deprotecting reagent. The method involves removing one or more of the non-required products of the deprotection reaction from the reactive array elements at which they are produced during the reaction, in order to displace the deprotection reaction towards completion.
专利号:WO-2007003236-A1 优先权日:2005-06-30 标 题:Process for synthesis of complex 2-deoxy-2-iodo pyranosides of high purity, particularly suitable for manufacturing pharmaceutically pure annamycin 发明人:SZEJA WIESLAW; GRYNKIEWICZ GRZEGORZ; FOKT IZABELA 权利人:ZACLAD BADAWCZO PROD SYNTEX; SZEJA WIESLAW; GRYNKIEWICZ GRZEGORZ; FOKT IZABELA 摘要:The method according to the invention comprises using as glycosyl donors high purity 2- deoxy-2-iodo derivatives of sugars of a defined configuration of C-2 carbon with O-alkyl, S- alkyl, O-aryl, S-aryl, O-heteroaryl, S-heteroaryl, O-acyl, O-silyl, O-N-imido, O-P- (phosphino, phosphono, thiophosphono, selenophosphono) groups at the anomeric position, and subjecting them to a condensation reaction with a compound containing a hydroxyl group or a protected hydroxyl group in the presence of electrophilic reagents, followed by deprotection and isolation of a pharmaceutically pure product. The objective of the present invention is to provide a method for preparing complex glycosides by coupling cyclic multifunctional compounds containing hydroxyl functional groups (glycosyl acceptors, including aglycones of natural origin which are known as constituents of active pharmaceutical ingredients) with diastereoisomerically pure 2-deoxy-2-halopyranosyl derivatives containing anomeric substituent capable of exchange under glycosidating conditions, for example by virtue of activation with electrophilic agents. This method substantially simplifies the synthesis of Annamycin. The present invention relies on a regio- and stereoselective reaction of cohalogenating 1,2- unsaturated sugars in the presence of hydroxyl group containing compounds, such as: water, alcohols, phenols, carboxylic acids, silanols, phosphinic acids, phosphoric acids, thiophosphoric acids, selenophosphoric acids, followed by separation of the product with proper C-2 carbon configuration required for the synthesis. As the separation of stereoisomers is carried out at the stage of obtaining a relatively inexpensive intermediate in the form of glycosyl donor, the method of the invention substantially reduces the cost of Annamycin manufacture. Other advantages of the synthesis process of the invention consist in the reduction of the number of stages of the antibiotic manufacture process and in yield increase of the final product.
专利号:WO-2024013633-A1 优先权日:2022-07-11 标 题 :Process for the synthesis of vitamin k2 发明人:SHASTRI MAYANK; BAIKAR MRUNALI H; VORA PARIN K; BNS RAJU 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to the synthesis of Vitamin K2 bearing varying prenyl side chains. The synthesis comprises the reaction of phenyl sulfone of tert-butyl dimethyl silyl (TBDMS) protected mono prenyl menadiol with prenyl halides bearing varying prenyl units in the presence of the phase transfer catalyst followed by reductive desulphonation to yield TBDMS ether of Vitamin K2. The TBDMS ether is then oxidized in the presence of chromium trioxide and periodic acid to yield the corresponding Vitamin K2.
专利号:US-2005101763-A1 优先权日:2003-09-30 标 题 :Synthesis of photolabile 2-(2-nitrophenyl)propyloxycarbonyl protected amino acids 发明人:DELISI CHARLES P; LAURSEN RICHARD A; BHUSHAN KUMAR R 权利人:UNIV BOSTON 摘要:The 2-(2-nitrophenyl)propyloxycarbonyl (NPPOC) group has been introduced as a photolabile amino protecting group for amino acids to be used as building blocks in photolithographic solid-phase peptide synthesis. NPPOC-protected amino acids were found to be cleaved in the presence of UV light about twice as fast as the corresponding o-nitroveratryloxycarbonyl (NVOC)-protected amino acids. The protected amino acids are of particular use in the synthesis of peptide arrays.
专利号:US-7872160-B2 优先权日:2008-03-31 标题:Single pot process for the regioselective synthesis of neolignan framework asarones 发明人:UPPULURI VENKATA MALLAVADHANI; AKELLA VENKATA SUBRAHMANYA SUDHAKAR; MAHAPATRA ANITA 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a single pot process for the regioselective synthesis of neolignan framework [3(R)-Ethyl-2(S)-methyl-3-(2″,4″,5″-trimethoxyphenyl)-1-(2′,4′,5′-trimethoxyphenyl)propane from toxic β-isomer rich asarone using montmorillonite acidic clay by employing microwave organic reaction enhancement (MORE) chemistry. This may be useful as versatile synthetic protocol for the synthesis of a large number of lignan and neolignan frameworks.
专利号:EP-0842924-B1 优先权日:1996-11-14 标 题 :Pyridine intermediates, useful in the synthesis of beta-adrenergic receptor agonists 发明人:WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:The present invention relates to certain compounds of the formula (I), which are useful in the synthesis of certain beta -adrenergic receptor agonists. The invention also relates to a process for synthesizing the compounds of formula (I) and to compounds of the formula (II), wherein R<1>, R<2> and R<4> are defined herein, which are useful in the synthesis of the compounds of formula (I). The invention also relates to a process for synthesizing a compound of formula (II). The invention further relates to processes for synthesizing compounds of formula (Z*), R<1>, R<2> and Y<2*> are defined herein.o
参考文献:10.1107/s1600536811010981 摘要:Choi HD, Seo PJ, Son BW, Lee U. 1-Cyclo-hexyl-sulfinyl-2-methyl-naphtho-[2,1-b]furan. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o1002. 参考文献:10.1107/s1600536811008270 摘要:Choi HD, Seo PJ, Son BW, Lee U. 5-Chloro-3-cyclo-hexyl-sulfonyl-2-methyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o828. 参考文献:10.1107/s1600536811008580 摘要:Choi HD, Seo PJ, Son BW, Lee U. 3-Cyclo-hexyl-sulfonyl-5-fluoro-2-methyl-1-benzofuran. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o847. 参考文献:10.1107/s1600536811009561 摘要:Benharref A, Lassaba E, Mazoir N, Daran JC, Berraho M. 7-Hy-droxy-8-isopropyl-1,1,4a-trimethyl-4a,9,10,10a-tetra-hydro-phenanthren-2(1H)-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o906. 参考文献:10.1107/s1600536811010452 摘要:Tebbaa M, Benharref A, Berraho M, Daran JC, Akssira M, Elhakmaoui A. 1-(4a,8-Dimethyl-1,2,3,4,4a,5,6,8a-octa-hydro-naphthalen-2-yl)-3-phenyl-prop-2-en-1-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o969.