4-氯-3-硝基苯甲酸置于palladium On Activated Charcoal,水,氢气,Sodium Hydroxide体系中,用 甲醇 用作溶剂,20.0~100.0 °C,101.33 Kpa 条件下,反应生成3-氨基-4-羟基苯甲酸 参考文献: Novel Arylalkene Derivatives And Use Thereof As Selective Estrogen Receptor Modulators[fr] Nouveaux Dérivés D'Arylalcène Et Utilisation De Ceux-Ci En Tant Que Modulateurs Sélectifs De Récepteur D'Oestrogène 标题: Novel Arylalkene Derivatives And Use Thereof As Selective Estrogen Receptor Modulators[fr] Nouveaux Dérivés D'Arylalcène Et Utilisation De Ceux-Ci En Tant Que Modulateurs Sélectifs De Récepteur D'Oestrogène 摘要:该发明提供了一种新型的乙烯衍生物,其化学式为i,可用作选择性雌激素受体调节剂(serms),并在预防和/或治疗依赖雌激素的疾病或症状方面具有用处.
专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
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-2014183560-A1 优先权日:2013-05-16 标题 :Afatinib and preparation method of intermediate thereof 发明人:XU XUENONG 权利人:SUZHOU MIRACPHARMA TECHNOLOGY CO LTD; XU XUENONG 摘要:Disclosed are a compound of 6-amino-7-hydroxy-3,4-dihydroquinazolin-4-one (I) which can be used in the preparation of Afatinib and the preparation method thereof, the method comprising the following steps: using 3-amino-4-hydroxy benzoic acid or 3-amino-4-hydroxy benzoate or 3-amino-4-hydroxy benzamide as raw materials to prepare the target compound (I) via nitration, reduction and cyclization reactions successively. At the same time, the present invention also reveals two synthesis routes which use compound (I) as a raw material to prepare Afatinib. The preparation and use of compound (I) make the synthesis of Afatinib more simple and environmental, and the yield and quality are improved, thus facilitating industrialization.
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-5527824-A 优先权日:1985-07-22 标题 :Substituted Di-T-Butlyphenols useful for inhibiting leukotriene synthesis 发明人:SCHERRER ROBERT A 权利人:RIKER LABORATORIES INC 摘要:Substituted Di-T-Butylphenols useful for inhibiting the synthesis of leukotrienes are disclosed.
专利号:WO-2025123424-A1 优先权日:2023-12-15 标 题 :Engineered bacterium for producing ansamitocin as well as construction method therefor and use thereof 发明人:WANG XINRAN; CHEN NINGXIN; LUO XIAOZHOU; JAY D KEASLING 权利人:SHENZHEN INST OF ADV TECH CAS 摘要:The present invention relates to an engineered bacterium for producing ansamitocin as well as a construction method therefor and the use thereof. The engineered bacterium overexpresses a FtsH protein. No study has reported the relationship between FtsH and ansamitocin. The present invention finds that the cell division protein FtsH is related to the synthesis of ansamitocin, and overexpressing FtsH can increase the yield of ansamitocin, thus saving the cost of industrial production of ansamitocin and increasing the fermentation efficiency. Therefore, the present invention is of great significance for realizing the industrial development of anti-tumor drugs in China, expanding the application range, and promoting clinical diagnosis and treatment of cancers.
[参考文献]: Chao-Bin Xue, Et Al. 3D-Qsar And Molecular Docking Studies Of Benzaldehyde Thiosemicarbazone, Benzaldehyde, Benzoic Acid, And Their Derivatives As Phenoloxidase Inhibitors. Bioorg Med Chem. 2007 Mar 1;15(5):2006-15. [参考文献]: Hirokazu Suzuki, Et Al. Arylamine N-Acetyltransferase Responsible For Acetylation Of 2-Aminophenols In Streptomyces Griseus. J Bacteriol. 2007 Mar;189(5):2155-9. [参考文献]: Hirokazu Suzuki, Et Al. Gric And Grid Constitute A Carboxylic Acid Reductase Involved In Grixazone Biosynthesis In Streptomyces Griseus. J Antibiot (Tokyo). 2007 Jun;60(6):380-7. [参考文献]: Hirokazu Suzuki, Et Al. Novel Benzene Ring Biosynthesis From C(3) And C(4) Primary Metabolites By Two Enzymes. J Biol Chem. 2006 Dec 1;281(48):36944-51.
合成参考文献
摘要:Schnürch, M.; Hämmerle, J.; Stanetty, P., Science of Synthesis Knowledge Updates, (2010) 1, 165. 摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198