专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-2002192767-A1 优先权日:1999-10-13 标题 :Biosynthesis of polyketide synthase substrates 发明人:KHOSLA CHAITAN; PFEIFER BLAINE 摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. coli . Production can be enhanced in microbial organisms of polyketides and other secondary metabolites by delaying production until after exponential phase and by maintaining relatively constant nutrient levels in the medium. In addition, polyketide production can be enhanced by providing an expression system for a thioesterase II. Thus, by modifying the host organism and changing the culture conditions, synthesis of a secondary metabolite can be enhanced. The present invention also results in a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.
专利号:WO-02068613-A1 优先权日:2001-02-28 标题 :Biosynthesis of polyketide synthase substrates 发明人:KHOSLA CHAITAN; PFEIFER BLAINE 权利人:UNIV LELAND STANFORD JUNIOR; KHOSLA CHAITAN; PFEIFER BLAINE 摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. coli. Production can be enhanced in microbial organisms of polyketides and other secondary metabolites by delaying production until after exponential phase and by maintaining relatively constant nutrient levels in the medium. In addition, polyketide production can be enhanced by providing an expression system for a thioesterase II. Thus, by modifying the host organism and changing the culture conditions, synthesis of a secondary metabolite can be enhanced. The present invention also results in a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.
专利号:US-4405523-A 优先权日:1982-03-24 标题:Process for preparation of benzophenone, anthraquinone and O-dibenzoylbenzene 发明人:FIELDS ELLIS K 权利人:STANDARD OIL CO INDIANA 摘要:Process for the concurrent synthesis of benzophenone, anthraquinone, and o-dibenzoylbenzene by pyrolysis of benzoic acid salts of yttrium, erbium, and dysprosium and mixtures thereof at temperatures of from about 200 DEG C. to 500 DEG C. and a pressure of about 0.1 to about 100 atmospheres. In an alternative method, a benzoic acid compound is passed through an oxide of yttrium, erbium, dysprosium and mixtures thereof in the presence of steam.
专利号:US-2002045220-A1 优先权日:1999-10-13 标题:Biosynthesis of polyketide synthase substrates 发明人:KHOSLA CHAITAN; PFEIFER BLAINE 摘要:The use of enzymes which catalyze the production of starter and extender units for polyketides is described. In addition, modified loading modules are described, which can accept a variety of starting units such as substituted benzoates, and which can be used to generate substituted derivatives of natural products. These enzymes may be used to enhance the yield of polyketides that are natively produced or polyketides that are rationally designed. By using these techniques, the synthesis of a complete polyketide has been achieved in E. col. This achievement permits a host organism with desirable characteristics to be used in the production of such polyketides and to assess the results of gene shuffling.
专利号:US-9050586-B2 优先权日:2012-03-13 标 题:Enantioselective organic anhydride reactions 发明人:CONNON STEPHEN J; TALLON SEAN; CORNAGGIA CLAUDIO; MANONI FRANCESCO; TORRENTE ESTHER 权利人:CONNON STEPHEN J; TALLON SEAN; CORNAGGIA CLAUDIO; MANONI FRANCESCO; TORRENTE ESTHER; PROVOST FELLOWS & SCHOLARS COLLEGE OF THE HOLY UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN 摘要:Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C 4 -C 50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.
参考文献:10.1107/s1600536811008403 摘要:Al-Eryani WF, Srinivasa HT, Jeyaseelan S, Sadashivaiah T, Devarajegowda HC. 4-(Benz-yloxy)phenyl 4-hexa-dec-yloxy-3-meth-oxy-benzoate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o840. 参考文献:10.1107/s1600536811012074 摘要:Kar S, Garai A, Bala S, Purohit CS. Tetrakis(μ-3-methoxybenzoato-κ2O1:O1′)bis[acetonitrilecopper(II)]. Acta Crystallogr E Struct Rep Online. 2011 Apr 07;67(5):m557. doi: 10.1107/s1600536811012074. 参考文献:10.4268/cjcmm20110712 摘要:Wu X, Lin S, Zhu C, Zhao F, Yu Y, Yue Z, Liu B, Yang Y, Dai J, Shi J. [Studies on constituents of cultures of fungus Phellinus igniarius]. Zhongguo Zhong Yao Za Zhi. 2011 Apr;36(7):874–80.