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

Sumatriptan CAS Registry Number: 103628-46-2 舒马曲坦

CAS Name: 3-[2-(Dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamidePercent Composition: C 56.92%, H 7.17%, N 14.22%, O 10.83%, S 10.85%
Literature References: Serotonin 5HT1-receptor agonist. Prepn: M. D. Dowle, I. H. Coates, DE 3320521; eidem, US 4816470; A. W. Oxford, GB 2162522 (1983, 1989, 1986 all to Glaxo). Receptor binding studies: P. P. A. Humphrey et al., Br. J. Pharmacol. 94, 1123 (1988); P. Schoeffter, D. Hoyer, Arch. Pharmacol. 340, 135 (1989). LC-MS determn in plasma: J. Oxford, M. S. Lant, J. Chromatogr. 496, 137 (1989). Clinical evaluations in migraine: A. Doenicke et al., Lancet 1, 1309 (1988); Subcutaneous Sumatriptan International Study Group, N. Engl. J. Med. 325, 316 (1991); in acute cluster headache: Sumatriptan Cluster Headache Study Group, ibid. 322. Review of pharmacology and clinical experience: S. J. Peroutka, Headache 30 (Suppl. 2), 554-560 (1990).

Cilansetron CAS Registry Number: 120635-74-7 西兰司琼

CAS Name: (10R)-5,6,9,10-Tetrahydro-10-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-pyrido[3,2,1-jk]carbazol-11(8H)-one
Additional Names: l-10[(2-methyl-1H-imidazol-1-yl)methyl]-5,6,8,9,10,11-hexahyd...
Literature References: Serotonin 5-HT3 receptor antagonist. Prepn: H. H. Haeck et al., EP 297651; eidem, US 4939136 (1989, 1990 both to Duphar Int. Res.); I. van Wijngaarden et al., J. Med. Chem. 36, 3693 (1993). Absolute configuration studies: P. G. Jones et al., Acta Crystallogr. E59, o38, o41 (2003). Pharmacology: A. Botella et al., Fundam. Clin. Pharmacol. 12, 619 (1998). Mechanism of action study: K. Hillsley et al., Neurosci. Lett. 278, 137 (2000). Clinical pharmacology: G. Stacher et al., Br. J. Clin. Pharmacol. 49, 429 (2000). Review of development and therapeutic potential: idem, Curr. Opin. Invest. Drugs 2, 1432-1436 (2001); of clinical experience: W. D. Chey, B. D. Cash, Expert Opin. Invest. Drugs 14, 185-193 (2005).

Palonosetron CAS Registry Number: 135729-61-2 帕洛诺司琼

CAS Name: (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
Percent Composition: C 76.99%, H 8.16%, N 9.45%, O 5.40%
Literature References: Serotonin 5-HT3 receptor antagonist. Prepn: J. Berger et al., EP 430190; eidem, US 5202333 (1991, 1993 both to Syntex); R. D. Clark et al., J. Med. Chem. 36, 2645 (1993). Improved synthesis: B. A. Kowalczyk, Heterocycles 43, 1439 (1996). Receptor binding study: E. H. F. Wong et al., Br. J. Pharmacol. 114, 851 (1995). Pharmacology: R. M. Eglen et al., ibid. 860. Clinical efficacy and pharmacokinetics: P. Eisenberg et al., Ann. Oncol. 15, 330 (2004). Clinical trial in prevention of chemotherapy-induced nausea and vomiting: R. Gralla et al., Ann. Oncol. 14, 1570 (2003). Review of pharmacology and clinical experience: S. M. Grunberg, J. M. Koeller, Expert. Opin. Pharmacother. 4, 2297-2303 (2003); M. A. A. Siddiqui, L. J. Scott, Drugs 64, 1125-1132 (2004).

Azasetron CAS Registry Number: 123040-69-7 盐酸阿扎司琼

CAS Name: N-1-Azabicyclo[2.2.2]oct-3-yl-6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxamide
Additional Names: (±)-6-chloro-3,4-dihydro-4-methyl-3-oxo-N-(3-quinuclidinyl)-2...
Literature References: Serotonin 5-HT3 receptor antagonist. Prepn: T. Tahara et al., EP 313393; eidem, US 4892872 (1989, 1990 both to Yoshitomi); T. Kawakita et al., Chem. Pharm. Bull. 40, 624 (1992). Receptor binding study: N. Sato et al., Jpn. J. Pharmacol. 59, 443 (1992). Pharmacology: K. Haga et al., ibid. 63, 377 (1993). Toxicity study: S. Takagi et al., Oyo Yakuri 42, 255 (1991), C.A. 117, 40208q (1991).

Alosetron CAS Registry Number: 122852-42-0 阿洛司琼

CAS Name: 2,3,4,5-Tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-1H-pyrido[4,3-b]indol-1-onePercent Composition: C 69.37%, H 6.16%, N 19.03%, O 5.44%
Literature References: Serotonin 5HT3-receptor antagonist. Prepn: I. H. Coates et al., EP 306323; eidem, US 5360800 (1989, 1994 both to Glaxo); of isotopically labelled compd: S. R. Prakash et al., J. Labelled Compd. Radiopharm. 36, 993 (1995). HPLC determn in plasma: T. L. Lloyd et al., J. Chromatogr. B 678, 261 (1996). Review of clinical pharmacology: M. D. Gunput, Aliment. Pharmacol. Ther. 13, Suppl. 2, 70-76 (1999); of clinical studies: A. W. Mangel, A. R. Northcutt, ibid. 77-82. Clinical trial in irritable bowel syndrome: M. Camilleri et al., Lancet 355, 1035 (2000).

Cisapride CAS Registry Number: 81098-60-4 西沙必利

CAS Name: cis-4-Amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxybenzamide
Additional Names: cis-4-amino-5-chloro-N-[1-[3-(p-fluorophenoxy)propyl]-3-methoxy-4-p...
Literature References: Serotonin 5-HT4 receptor agonist. Prepn: G. Van Daele, EP 76530; idem, US 4962115 (1983, 1990 both to Janssen); and pharmacology: idem et al., Drug Dev. Res. 8, 225 (1986). Pharmacokinetics: J. A. Barone et al., Clin. Pharm. 6, 640 (1987). Review of pharmacology and therapeutic efficacy: L. R. Wiseman, D. Faulds, Drugs 47, 116-152 (1994).

Metergoline CAS Registry Number: 17692-51-2 甲麦角林

CAS Name: [[(8b)-1,6-Dimethylergolin-8-yl]methyl]carbamic acid phenylmethyl ester
Additional Names: D-8b-[(carbobenzoxyamino)methyl]-1,6-dimethyl-10a-ergoline; D-N-carbobenzoxydihydro-1-methyll...
Literature References: Serotonin 5HT-receptor antagonist. Prepn: Bernardi et al., Gazz. Chim. Ital. 94, 936 (1964); Camerino et al., US 3238211 (1966 to Farmitalia). Pharmacology: C. Beretta et al., Nature 207, 421 (1965). Metabolic studies: Arcamone et al., Boll. Chim. Farm. 110, 704 (1971). Mode of action study: L. Krulich et al., Endocrinology 108, 1115 (1981). Clinical antiprolactin activity: F. Scapin et al., Eur. J. Clin. Pharmacol. 22, 181 (1982); A. Caballero et al., J. Reprod. Med. 32, 115 (1987).

Sibutramine CAS Registry Number: 106650-56-0 西布曲明

CAS Name: 1-(4-Chlorophenyl)-N,N-dimethyl-a-(2-methylpropyl)cyclobutanemethanamine
Additional Names: N-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl-N,N-dimethylamine
Percent Composition: C...
Literature References: Serotonin and noradrenaline reuptake inhibitor (SNRI); decreases calorie intake and increases energy expenditure. Prepn: J. E. Jeffery et al., DE 3212682; idem, US 4929629 (1982, 1990 both to Boots). Clinical trial in obesity: C. Hanotin et al., Int. J. Obes. 22, 32 (1998). Review of pharmacology and mechanism of action: D. J. Heal et al., ibid., Suppl. 1, S18-S28.

Milnacipran CAS Registry Number: 92623-85-3 米那普仑

CAS Name: (1R,2S)-rel-2-(Aminomethyl)-N,N-diethyl-1-phenylcyclopropanecarboxamide
Additional Names: 1-phenyl-1-(diethylaminocarbonyl)-2-(aminomethyl)cyclopropane; midalcipran
Percent Composi...
Literature References: Serotonin and norepinephrine reuptake inhibitor (SNRI). Prepn: G. Mouzin et al., EP 68999; eidem, US 4478836 (1983, 1984 both to Pierre Fabre); B. Bonnaud et al., J. Med. Chem. 30, 318 (1987). Mechanism of action study: C. Moret et al., Neuropharmacology 24, 1211 (1985). Clinical inhibition of monoamine uptake: C. Palmier et al., Eur. J. Clin. Pharmacol. 37, 235 (1989). Review of pharmacology and clinical efficacy in depression: C. M. Spencer, M. I. Wilde, Drugs 56, 405-427 (1998).

Fonazine CAS Registry Number: 7456-24-8 二甲替嗪

CAS Name: 10-[2-(Dimethylamino)propyl]-N,N-dimethyl-10H-phenothiazine-2-sulfonamide
Additional Names: 10-(2-dimethylaminopropyl)-3-dimethylsulfamidophenothiazine; 3-dimethylsulfamido-10-(2-dime...
Literature References: Serotonin inhibitor. Prepn: GB 814512 (1959 to Rhône-Poulenc). Pharmacokinetics and distribution in dog and rat: O. R. W. Lewellen, R. Templeton, Adv. Biochem. Psychopharmacol. 9, 213 (1974). Clinical evaluation in spasticity: W. B. Matthews et al., Acta Neurol. Scand. 48, 635 (1972). HPLC determn in plasma: J. Holt et al., Br. J. Clin. Pharmacol. 13, 282 (1982).