其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Dithiopyr CAS Registry Number: 97886-45-8 氟氯草定

CAS Name: 2-(Difluoromethyl)-4-(2-methylpropyl)-6-(trifluoromethyl)-3,5-pyridinedicarbothioic acid S,S-dimethyl ester
Additional Names: S,S-dimethyl 2-(difluoromethyl)-4-isobutyl-6-trifluoromet...
Literature References: Selective herbicide for weed control in turfgrass and selected crops. Prepn: L. F. Lee, EP 133612; idem, US 4692184 (1985, 1987 both to Monsanto). Herbicidal properties: M. Fujiyama, S. Yamane, Shokubutsu no Kagaku Chosetsu 24, 49 (1989), C.A. 111, 227154n (1989).

Saquinavir CAS Registry Number: 127779-20-8 沙奎那韦

CAS Name: (2S)-N1[(1S,2R)-3-[(3S,4aS,8aS)-3-[[(1,1-Dimethylethyl)amino]carbonyl]octahydro-2(1H)-isoquinolinyl]-2-hydroxy-1-(phenylmethyl)propyl]-2-[(2-quinolinylcarbonyl)amino]butanediamide
Add...
Literature References: Selective HIV protease inhibitor. Prepn: J. A. Martin, S. Redshaw, EP 432695; eidem, US 5196438 (1991, 1993 both to Hoffmann-LaRoche); K. E. B. Parkes et al., J. Org. Chem. 59, 3656 (1994). In vitro HIV proteinase inhibition: N. A. Roberts et al., Science 248, 358 (1990). Antiviral properties: J. C. Craig et al., Antiviral Res. 16, 295 (1991); S. Galpin et al., Antiviral Chem. Chemother. 5, 43-45 (1994). Clinical evaluation of tolerability and activity: V. S. Kitchen et al., Lancet 345, 952 (1995). Review of pharmacology and clinical experience: S. Kravcik, Expert Opin. Pharmacother. 2 303-315 (2001).

Sitagliptin CAS Registry Number: 486460-32-6 西他列汀

CAS Name: 7-[(3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine
Additional Names: (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihy...
Literature References: Selective inhibitor of dipeptidyl peptidase IV (DPP-IV). Prepn: S. D. Edmondson et al., WO 03004498; eidem, US 6699871 (2003, 2004 both to Merck Co.); and enzyme inhibitory profile: D. Kim et al., J. Med. Chem. 48, 141 (2005). Improved process: K. B. Hansen et al., Org. Process Res. Dev. 9, 634 (2005). Clinical pharmacokinetics and pharmacodynamics: G. A. Herman et al., Clin. Pharmacol. Ther. 78, 675 (2005). Review: C. F. Deacon, Curr. Opin. Invest. Drugs 6, 419-426 (2005).

Buthionine Sulfoximine CAS Registry Number: 5072-26-4 D,L-蛋氨酸-(S,R)-亚磺酰亚胺

CAS Name: 2-Amino-4-(S-butylsulfonimidoyl)butanoic acid
Additional Names: S-(3-amino-3-carboxypropyl)-S-butylsulfoximine; S-(n-butyl)homocysteine sulfoximine; BSO
Percent Composition: C 43.2...
Literature References: Selective inhibitor of g-glutamyl cysteine synthetase, an enzyme in the glutathione, q.v., biosynthetic pathway. BSO-mediated depletion of intracellular glutathione has been associated with increased sensitivity of tumor cells to antineoplastic agents. Prepn: K. Hayashi, Chem. Pharm. Bull. 8, 177 (1960). Synthesis and in vitro and in vivo enzyme inhibition: O. W. Griffith, A. Meister, J. Biol. Chem. 254, 7758 (1979). Mechanism of action and metabolism in animals O. W. Griffith, ibid. 257, 13704 (1982). Chemosensitization by BSO of melphalan-resistant murine leukemia cells in vivo: S. Somfai-Relle et al., Biochem. Pharmacol. 33, 485 (1984); R. A. Kramer et al., Cancer Res. 47, 1593 (1987). Enhanced melphalan, q.v., cytotoxicity in human cancer cells in vitro: J. A. Green et al., ibid. 44, 5427 (1984); and in mice bearing human tumor xenografts: H. S. Friedman et al., J. Natl. Cancer Inst. 81, 524 (1989).

Suplatast Tosylate CAS Registry Number: 94055-76-2 甲磺司特

CAS Name: [3-[[4-(3-Ethoxy-2-hydroxypropoxy)phenyl]amino]-3-oxopropyl]dimethylsulfonium salt with 4-methylbenzenesulfonic acid
Additional Names: (±)-[2-[[p-(3-ethoxy-2-hydroxypropoxy)pheny...
Literature References: Selective inhibitor of the IgE antibody response; inhibits interleukin-4 gene expression and mast cell differentiation. Prepn: A. Koda et al., DE 3408708; eidem, US 4556737 (1984, 1985 both to Taiho). Suppression of IL-4 production and the IgE response: Y. Yanagihara et al., Jpn. J. Pharmacol. 61, 23, 31 (1993). Effect on mast cell differentiation: S. Konno et al., Eur. J. Pharmacol. 259, 15 (1994). Series of articles on toxicology: J. Toxicol. Sci. 17, Suppl. 2, 1-205, (1992); C.A. 117, 103839-103846; 103995 (1992). Acute toxicity: K. Yamishita et al., ibid. 1. Clinical evaluation in asthma: J. Tamaoki et al., Lancet 356, 273 (2000).

Cariporide CAS Registry Number: 159138-80-4 卡立泊来德

CAS Name: N-(Aminoiminomethyl)-4-(1-methylethyl)-3-(methylsulfonyl)benzamide
Additional Names: 4-isopropyl-3-(methanesulfonylbenzoyl)guanidine
Percent Composition: C 50.87%, H 6.05%, N 14.83...
Literature References: Selective inhibitor of the sodium-hydrogen exchanger subtype 1 (NHE-1); protects against myocardial injury following ischemia and reperfusion. Prepn: H. J. Lang et al., EP 589336; eidem, US 5591754 (1994, 1997 both to Hoechst); A. Weichert et al., Arzneim.-Forsch. 47, 1204 (1997). Pharmacology: W. Scholz et al., Cardiovasc. Res. 29, 260 (1995). Symposium on pharmacology and clinical experience: Am. J. Cardiol. 83, Suppl. 10A, 1G-25G (1999). Review: W. Scholz et al., J. Thromb. Thrombolysis 8, 61-70 (1999).

Thalidomide CAS Registry Number: 50-35-1 沙利度胺

CAS Name: 2-(2,6-Dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione
Additional Names: N-(2,6-dioxo-3-piperidyl)phthalimide; a-phthalimidoglutarimide; 3-phthalimidoglutarimide; 2,6-dioxo-3-phthalim...
Literature References: Selective inhibitor of tumor necrosis factor a (TNF-a). Formerly used as sedative, hypnotic. Prepn: GB 768821 (1957 to Chemie Grünenthal). Teratogenicity studies: I. D. Fratta et al., Toxicol. Appl. Pharmacol. 7, 268 (1965). Review of proposed mechanisms of embryopathy: T. D. Stephens, Teratology 38, 229-239 (1988). HPLC determn in plasma: A. Delon et al., J. Liq. Chromatogr. 18, 297 (1995). Stereospecific determn and pharmacokinetics of enantiomers: T. Eriksson et al., Chirality 7, 44 (1995). Clinical trial in HIV wasting syndrome: G. Reyes-Terán et al., AIDS 10, 1501 (1996); in aphthous ulcers related to HIV infection: J. M. Jacobson et al., N. Engl. J. Med. 336, 1487 (1997). Review of chemistry, pharmacokinetics and clinical safety: V. Günzler, Drug Saf. 7, 116-134 (1992); of effect on TNF-a and clinical use in leprosy and tuberculosis: J. D. Klausner et al., Clin. Immunol. Immunopathol. 81, 219-223 (1996); of pharmacology, history and potential clinical uses: D. Stirling et al., J. Am. Pharm. Assoc. NS37, 307-313 (1997); of use in multiple myeloma: S. V. Rajkumar, Expert Rev. Anticancer Ther.1, 20-28 (2001); of pharmacology and toxicology: C. Meierhofer, C. J. Wiedermann, Curr. Opin. Drug Disc. Devel. 6, 92-99 (2003); of clinical experience: S. J. Matthews, C. McCoy, Clin. Ther. 25, 342-395 (2003).

Prinomastat CAS Registry Number: 192329-42-3 普马司他

CAS Name: (3S)-N-Hydroxy-2,2-dimethyl-4-[[4-(4-pyridinyloxy)phenyl]sulfonyl]-3-thiomorpholinecarboxamide
Additional Names: 3(S)-N-hydroxy-4-((4-((pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl)te...
Literature References: Selective matrix metalloproteinase inhibitor with antiangiogenic activity. Prepn: S. E. Zook et al., WO 9720824; S. L. Bender, M. J. Melnick, US 5753653 (1997, 1998 both to Agouron). Pharmacokinetic and antitumor efficacy in rats: O. Santos et al., Clin. Exp. Metastasis 15, 499 (1997). Review of pharmacology: D. R. Shalinsky et al., Ann. N.Y. Acad. Sci. 878, 236-270 (1999); and clinical experiences: R. Scatena, Expert Opin. Invest. Drugs 9, 2159-2165 (2000).

Xanomeline CAS Registry Number: 131986-45-3 占诺美林

CAS Name: 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine
Percent Composition: C 59.75%, H 8.24%, N 14.93%, O 5.69%, S 11.39%
Literature References: Selective muscarinic M1-receptor agonist. Prepn: P. Sauerberg, P. H. Olesen, EP 384288 (1990 to Ferrosan); eidem, US 5043345 (1991 to Novo Nordisk); eidem et al., J. Med. Chem. 35, 2274 (1992). Prepn of crystalline tartrate: L. M. Osborne et al., WO 9429303 (1994 to Novo Nordisk). Muscarinic receptor binding study: H. E. Shannon et al., J. Pharmacol. Exp. Ther. 269, 271 (1994). Pharmacology: F. P. Bymaster et al., ibid. 282. HPLC determn in plasma: C. L. Hamilton et al., J. Chromatogr. 613, 365 (1993).

Sabcomeline CAS Registry Number: 159912-53-5 沙可美林

CAS Name: R-(Z)-a-(Methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitrilePercent Composition: C 62.15%, H 7.82%, N 21.74%, O 8.28%
Literature References: Selective muscarinic M1-receptor partial agonist. Prepn: B. S. Orlek et al., EP 392803; eidem, US 5278170; (1990, 1994 both to Beecham); S. M. Bromidge et al., J. Med. Chem. 40, 4265 (1997). Pharmacology: J. M. Loudon et al., J. Pharmacol. Exp. Ther. 283, 1059 (1997). Cognition improvement in rats: H. Hodges et al., Behav. Brain Res. 99, 81 (1999).