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Pazopanib CAS# 444731-52-6 帕唑帕尼
Pazopanib is an approved drug, is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits vascular endothelial growth fac...
Boloor, Amogh; Cheung, Mui; Davis, Ronda; Harris, Philip Anthony; Hinkle, Kevin; Mook, Robert Anthony; Stafford, Jeffery Alan; Veal, James Martin. Preparation of pyrimidinamines as angiogenesis modulators. Assignee Glaxo Group Limited, UK. WO 2002059110. (2002).
Pelitrexol CAS# 446022-33-9 N-((5-(2-((6S)-2-氨基-1,4,5,6,7,8-六氢-4-氧代吡啶并[2,3-D]嘧啶-6-基)乙基)-4-甲基-2-噻吩)甲酰基)-L-谷氨酸
Pelitrexol (AG2034) is a potent antifolate thymidylate synthase (TS) inhibitor with demonstrated antitumor activity in vitro and in vivo. In enzyme and cell-based assays, pelitrexol inhibits TS with l...
1.1Reagents:Sulfuric acid;18 h, reflux; reflux → rt1.2Reagents:Sodium bicarbonate;pH 82.1Reagents:TriethylamineCatalysts:Cuprous iodide,Tetrakis(triphenylphosphine)palladiumSolvents:Acetonitrile;18 h, rt → 82 °C3.1Reagents:HydrogenCatalysts:PalladiumSolvents:Ethanol;10 d, 65 °C4.1Reagents:Lithium hydroxideSolvents:Tetrahydrofuran,Water;19 h, rt → 45 °C4.2Reagents:Hydrochloric acidSolvents:Water;pH 15.1Reagents:Potassium carbonateSolvents:Dimethylformamide;rt → 15 °C; overnight, 15 °C → rt6.1Reagents:Dipyridinium dichromateSolvents:Dimethylformamide;23 - 24 °C; overnight, 24 °C → rt6.2Reagents:Water6.3Reagents:Hydrochloric acidSolvents:Water;pH 3 - 47.1Reagents:TriethylamineSolvents:tert-Butyl methyl ether;rt → -16 °C7.2Reagents:Pivaloyl chloride;-16 °C → rt7.3Reagents:ButyllithiumSolvents:Tetrahydrofuran,Hexane;rt; 1 h, rt → -70 °C7.41 h, -70 °C7.5Reagents:Potassium bisulfateSolvents:Water8.1Reagents:Titanium tetrachlorideSolvents:Dichloromethane;1.25 h, 3 - 7 °C; 1 h, 3 - 7 °C8.2Reagents:Diisopropylethylamine;3 - 7 °C; 1 h, 3 - 7 °C; 7 °C → -70 °C8.3Solvents:Dichloromethane;30 min, -70 °C8.4Reagents:Titanium tetrachlorideSolvents:Dichloromethane;1.5 h, -70 °C; 1 h, -70 °C; 16 h, 4 °C8.5Reagents:Ammonium chlorideSolvents:Water8.1Reagents:Titanium tetrachlorideSolvents:Dichloromethane;1.25 h, 3 - 7 °C; 1 h, 3 - 7 °C8.2Reagents:Diisopropylethylamine;3 - 7 °C; 1 h, 3 - 7 °C; 7 °C → -70 °C8.3Solvents:Dichloromethane;30 min, -70 °C8.4Reagents:Titanium tetrachlorideSolvents:Dichloromethane;1.5 h, -70 °C; 1 h, -70 °C; 16 h, 4 °C8.5Reagents:Ammonium chlorideSolvents:Water9.1Reagents:Lithium borohydrideSolvents:Tetrahydrofuran,Water;rt; 2.5 h, rt9.2Reagents:Hydrochloric acidSolvents:Water10.1Reagents:TriethylamineSolvents:Dichloromethane;rt → -10.3 °C10.2-10.3 °C; 2.25 h, -10.3 °C10.3Reagents:Hydrochloric acidSolvents:Water11.1Reagents:Sodium hydride,Sodium iodideSolvents:Tetrahydrofuran;62 °C11.2Reagents:Sodium bicarbonateSolvents:tert-Butyl methyl ether,Water12.1Reagents:Hydrogen bromideSolvents:Acetic acid;15 h, rt12.2Solvents:Water;pH 8 - 9; pH 113.1Reagents:Lawesson's reagentSolvents:Tetrahydrofuran;21.5 h, 35 °C13.2Reagents:Sodium chlorideSolvents:Dichloromethane,Water14.1110 °C14.2Reagents:Hydrochloric acidSolvents:Water;pH 5 - 615.1Reagents:Triethylamine,2-Chloro-4,6-dimethoxy-1,3,5-triazineSolvents:Dimethylformamide;1.5 h, rt15.224 h, rt16.1Reagents:Trifluoroacetic acidSolvents:Dichloromethane;10 - 16 h, 0 °C
Desvenlafaxine Succinate CAS# 448904-47-0 去甲文拉法辛(O-去甲文拉法辛)琥珀酸
Desvenlafaxine Succinate is a venlafaxine metabolite and inhibitor of SERT and NET used to treat depression. It also alters rates of gastric emptying and decreases symptoms of menopausal hot flashes.
Wang, Peng; Cui, Xiangjuan; Liu, Weijia; Hai, Li; Zhongnan Yaoxue; Volume 10; Issue 3; Pages 175-177; Journal; 2012
Obeticholic acid CAS# 459789-99-2 奥贝胆酸
Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It i...
Reference: Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Maloney PR, Morelli A, Parks DJ, Willson TM. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002 Aug 15;45(17):3569-72. PubMed PMID: 12166927.
Plecanatide CAS# 467426-54-6 普卡那肽
Plecanatide (brand name Trulance), is a drug approved by the FDA for the treatment of chronic idiopathic constipation (CIC) and irritable bowel syndrome with constipation. Plecanatide is an agonist of...
Reference: Chen, Xue Ming; Zhu, Yan Ting; Mi, Peng Cheng; Tao, An Jin; Yuan, Jian Cheng. Preparation of plecanatide. WO 2018205401. (PCT Int. Appl. (2018))
Viloxazine CAS# 46817-91-8 维洛沙秦
Viloxazine is a selective norepinephrine reuptake inhibitor (NRI) with additional modulatory effects on serotonergic signaling. In preclinical transporter assays, it inhibited the norepinephrine trans...
Lewis acid mediated intramolecular C-O bond formation of alkanol-epoxide leading to substituted morpholine and 1,4-oxazepane derivatives: total synthesis of (±)-ViloxazineBy: Ghosh, Priya; et alTetrahedron (2016), 72(5), 690-698
Selexipag CAS# 475086-01-2 赛乐西帕
Selexipag, also known as ACT-293987 and NS-304, is a a first-in-class orally available selective non-prostanoid IP receptor agonist, which is currently in development by Actelion as a treatment of pul...
Reference: Chen, Fangjun; Deng, Zeping; Cheng, Jia; Xu, Hui; Tang, Liming. Selexipag intermediate 2-(4-bromobutoxy)acetic acid and 2-(4-bromobutoxy)-N-(methylsulfonyl)acetamide, and preparation method of selexipag. CN 108558653. (Hunan Huateng Pharmaceutical Co., Ltd., Peop. Rep. China)
Tivozanib CAS# 475108-18-0 替沃扎尼
Tivozanib (AV-951) is a potent, selective, orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. In preclinical kinase assays, it inhibited VEGFR2 with an ...
A new and practical synthesis of tivozanibBy: Zhu, Chunping; et alHeterocycles (2016), 92(10), 1882-1887
Eliglustat CAS# 491833-29-5 依利格鲁司特
Eliglustat, also known as GENZ-112638, (trade name Cerdelga) is a treatment for Gaucher's disease developed by Genzyme Corp that was approved by the FDA August 2014. Commonly used as the tartrate salt...
Sun, Guodong; Jian, Weilin; Luo, Zhonghua; Sun, Tengfei; Li, Chao; Zhang, Jiancun; Wang, Zhongqing. Development of an Efficient and Scalable Asymmetric Synthesis of Eliglustat via Ruthenium(II)-Catalyzed Asymmetric Transfer Hydrogenation. Organic Process Research & Development. Volume 23. Issue 6. Pages 1204-1212. Journal; Online Computer File. (2019).
Eltrombopag CAS# 496775-61-2 伊屈泼帕
Eltrombopag, also known as SB-497115-GR, is an agonist of the c-mpl (TpoR) receptor, which is the physiological target of the hormone thrombopoietin. Eltrombopag was initially approved in 2008, for ...
Preparation process of an agonist of the thrombopoietin receptor; Bartra Sanmarti, Marti; Solsona Rocabert, Joan Gabriel; Cruces Colado, Jacobo; Enjo Babio, Juan; Pampin Casal, Maria Begona; Assignee Esteve Quimica, S.A., Spain; Galchimia, S.L. 2014; Patent Information; Nov 05, 2014; EP 2799425 A1
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