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

Sultopride CAS Registry Number: 53583-79-2 舒托必利

CAS Name: N-[(1-Ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-2-methoxybenzamide
Additional Names: N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-o-anisamide
Percent Composition: C 57...
Literature References: Dopamine D2-receptor antagonist. Prepn: C. S. Miller et al., FR M 5916; see also: G. Bulteau et al., US 3975434 (1966, 1976 both to Soc. Etudes Sci. Ind. l'Ile-de-France). Pharmacology: C. Lavelle, J. Margarit, J. Pharmacol. 5, Suppl. 2, 58 (1974); B. Bruguerolle et al., ibid. 12, 27 (1981). Clinical trial in psychosis: D. Morel, Sem. Hop. 59, 2337 (1983). GC determn in serum: A. Kamizono et al., J. Chromatogr. 567, 113 (1991). Pharmacokinetics of enantiomers: idem et al., Biol. Pharm. Bull. 16, 1121 (1993).

Tetrabenazine CAS Registry Number: 58-46-8 丁苯那嗪

CAS Name: 1,3,4,6,7,11b-Hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a]quinolizin-2-one
Additional Names: 2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bH-benzo[a]quinolizineP...
Literature References: Dopamine depleting agent. Prepn: Brossi et al., Helv. Chim. Acta 41, 119 (1958); US 2830993 (1958 to Hoffmann-La Roche); Osbond, J. Chem. Soc. 1961, 4711. Pharmacology: Leusen et al., Arch. Int. Pharmacodyn. 119, 225 (1959). Metabolism: Schwartz et al., Biochem. Pharmacol. 15, 645 (1966). Clinical trials in hyperkinetic movement disorders: J. Janovic, Ann. Neurol. 11, 41 (1982); J. Janovic, J. Orman, Neurology 38, 391 (1988).

Docarpamine CAS Registry Number: 74639-40-0 朵卡派明

CAS Name: 4-[2-[[(2S)-2-(Acetylamino)-4-(methylthio)-1-oxobutyl]amino]ethyl]-1,2-phenylene diethyl ester
Additional Names: (-)-(S)-2-acetamido-N-(3,4-dihydroxyphenethyl)-4-(methylthio)butyramid...
Literature References: Dopamine prodrug. Prepn: T. Kiguchi et al., EP 7441; eidem, US 4228183 (both 1980 to Tanabe Seiyaku). Pharmacology: I. Yamaguchi et al., J. Cardiovasc. Pharmacol. 13, 879 (1989). Mechanism of action: S. Nishiyama et al., ibid. 14, 175 (1989). Pharmacokinetics: M. Yoshikawa et al., Drug Metab. Dispos. 16, 754 (1988). Metabolism in humans: eidem, ibid. 18, 212 (1990). HPLC determn in biological fluids: eidem, Biomed. Chromatogr. 4, 181 (1990). Review: S. Nishiyama et al., Cardiovasc. Drug Rev. 10, 101-116 (1992).

Dopexamine CAS Registry Number: 86197-47-9 多培沙明

CAS Name: 4-[2-[[6-[(2-Phenylethyl)amino]hexyl]amino]ethyl]-1,2-benzenediol
Additional Names: 4-[2-[[6-(phenethylamino)hexyl]amino]ethyl]pyrocatecholPercent Composition: C 74.12%, H 9.05%, N 7....
Literature References: Dopamine receptor and b2-adrenoreceptor agonist. Prepn: J. B. Farmer et al., EP 72061 (1983 to Fisons). Unlike dopamine, dopexamine has little or no activity at the a- and b1-adrenoceptors: R. A. Brown et al., Br. J. Pharmacol. 85, 599 (1985). Cardiovascular activity in dogs: eidem, ibid. 609. Hemodynamic effects in chronic congestive heart failure: J. R. Dawson et al., Br. Heart J. 54, 313 (1985); G. Svensson et al., Eur. Heart J. 7, 697 (1986). Human renovascular effects: F. Magrini et al., Eur. J. Clin. Pharmacol. 32, 1 (1987). Symposium on pharmacology and clinical efficacy: Am. J. Cardiol. 62, Suppl., 1C-88C (1988).

Clebopride CAS Registry Number: 55905-53-8 氯波必利

CAS Name: 4-Amino-5-chloro-2-methoxy-N-[1-(phenylmethyl)-4-piperidinyl]benzamide
Additional Names: 4-amino-N-(1-benzyl-4-piperidyl)-5-chloro-o-anisamide; N-(1'-benzyl-4'-piperidyl)-2-methoxy-4-...
Literature References: Dopamine receptor antagonist related to metoclopramide, q.v. Prepn: R. G. Spickett et al., DE 2513136; A. V. Noverola et al., US 4138492 (1975, 1979 both to Anphar); J. Prieto et al., J. Pharm. Pharmacol. 29, 147 (1977). Pharmacological study: J. L. Masso, D. J. Roberts, ibid. 32, 727 (1980). In vitro metabolism studies: G. Huizing et al., Xenobiotica 10, 211 (1980); G. Huizing, A. H. Beckett, ibid. 593. Pharmacokinetics: J. Segura et al., J. Pharm. Pharmacol. 33, 214 (1981). Comparative study of anti-emetic and gastrointestinal effects: P. Berga et al., Arch. Farmacol. Toxicol. 7, 189 (1981). Efficacy in healing exptl ulcers: Y. Matsuo et al., Oyo Yakuri 24, 251 (1982); S. Okabe et al., ibid. 261, C.A. 97, 208081n, 208082p (1982). Determn in urine and plasma by radioimmunoassay: M. Yano et al., Chem. Pharm. Bull. 32, 1491 (1984). Clinical effect in postoperative nausea: D. F. Duarte et al., Clin. Ther. 7, 365 (1985).

Mosapramine CAS Registry Number: 89419-40-9 莫沙帕明

CAS Name: 1'-[3-(3-Chloro-10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]hexahydrospiro[imidazo[1,2-a]pyridine-3(2H),4'-piperidin]-2-one
Additional Names: 1'-[3-(3-chloro-10,11-dihydro-5H-diben...
Literature References: Dopamine receptor antagonist with adrenoceptor blocking activity; metabolite of clocapramine, q.v. Prepn: C. Tashiro, I. Horii, US 4337260 (1982 to Yoshitomi); C. Tashiro et al., Yakugaku Zasshi 109, 93 (1989), C.A. 112, 35749j (1990). X-ray crystallographic analysis: I. Ueda, C. Tashiro, Acta Crystallogr. C40, 422 (1984). Receptor binding studies: M. Setoguchi et al., Eur. J. Pharmacol. 112, 313 (1985). Pharmacokinetics and metabolism: J. Ishigooka et al., Psychopharmacology 97, 303 (1989). Toxicity data: H. Horizoe et al., Oyo Yakuri 37, 529 (1989); C.A. 111, 167174g (1989). HPLC determn in plasma: K. Hikida et al., Anal. Sci. 6, 367 (1990).

Amisulpride CAS Registry Number: 71675-85-9 阿米舒必利

CAS Name: 4-Amino-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-2-methoxybenzamide
Additional Names: 4-amino-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-o-anisamide; aminosultop...
Literature References: Dopamine receptor antagonist. Prepn: M. Thominet et al., BE 872585; eidem, US 4401822 (1979, 1983 both to Soc. d'Etudes Sci. Ind. de l'Ile-de-France). Crystal structure: H. L. DeWinter et al., Acta Crystallogr. C46, 313 (1990). Psychopharmacology: G. Perrault et al., J. Pharmacol. Exp. Ther. 280, 73 (1997). HPLC determn in plasma and urine: B. Malavasi et al., J. Chromatogr. B 676, 107 (1996). Series of articles on pharmacology and clinical efficacy in schizophrenia: Int. Clin. Psychopharmacol. 12, Suppl. 2, S11-S36 (1997).

Thioridazine CAS Registry Number: 50-52-2 硫利达嗪

CAS Name: 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylthio)-10H-phenothiazine
Additional Names: 2-methylmercapto-10-[2-(N-methyl-2-piperidyl)ethyl]phenothiazine; 3-methylmercapto-N-[2'-(N'-me...
Literature References: Dopamine receptor blocker; parent compound of sulforidazine and mesoridazine, q.q.v. Prepn: Bourquin et al., Helv. Chim. Acta 41, 1072 (1958). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Effect on dopaminergic function: D. M. Niedzwiecki et al., J. Pharmacol. Exp. Ther. 228, 636 (1984); C. D. Kilts et al., ibid. 231, 334 (1984). GLC determn in plasma: E. C. Dinovo et al., J. Pharm. Sci. 65, 667 (1976). HPLC sepn of isomers: R. Whelpton et al., J. Chromatogr. 426, 223 (1988). Clinical evaluation: R. Axelsson et al., Curr. Ther. Res. 21, 587 (1977). Comprehensive description: E. M. Abdel-Moety, K. A. Al-Rashood, Anal. Profiles Drug Subs. 18, 459-525 (1989).

Mesoridazine CAS Registry Number: 5588-33-0 美索哒嗪

CAS Name: 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylsulfinyl)-10H-phenothiazine
Additional Names: thioridazine-2-sulfoxidePercent Composition: C 65.25%, H 6.78%, N 7.25%, O 4.14%, S 16.59%
Literature References: Dopamine receptor blocking agent; analog of thioridazine. Prepn: Renz et al., US 3084161 (1963 to Sandoz). Pharmacology and toxicology: Loew et al., Boll. Chim. Farm. 106, 332-371 (1967). Effects on dopaminergic function in comparison with sulforidazine and thioridazine, q.q.v.: D. M. Niedzwiecki et al., J. Pharmacol. Exp. Ther. 228, 636 (1984); C. D. Kilts et al., ibid. 231, 334 (1984). GLC determn in plasma: E. C. Dinovo et al., J. Pharm. Sci. 65, 667 (1976). Clinical evaluation in sleep disorders: K. Adam et al., Br. J. Clin. Pharmacol. 3, 157 (1976); as antipsychotic: R. Axelsson, Curr. Ther. Res. 21, 587 (1977). Toxicity studies: S. Maruyama et al., Niigata Igakkai Zasshi 81, 611 (1967), C.A. 68, 76856h (1968). Brief description: J. Am. Med. Assoc. 216, 313 (1971).

Aripiprazole CAS Registry Number: 129722-12-9 阿立哌唑

CAS Name: 7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone
Additional Names: 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyrilTrademarks:...
Literature References: Dopamine-serotonin system stabilizer. Exhibits partial agonist activity at dopamine D2-receptors and serotonin 5-HT1A-receptors and antagonist activity at 5-HT2A-receptors. Prepn: Y. Oshiro et al., EP 367141; eidem, US 5006528 (1990, 1991 both to Otsuka); and pharmacology: Y. Oshiro et al., J. Med. Chem. 41, 658 (1998). Description of action on dopamine receptors: S. M. Stahl, J. Clin. Psychiatry 62, 841, 923 (2001); on serotonin receptors: S. Jordan et al., Eur. J. Pharmacol. 441, 137 (2002). Clinical trial in schizophrenia: J. M. Kane et al., J. Clin. Psychiatry 63, 763 (2002). Review of pharmacology: J. K. McGavin, K. L. Goa, CNS Drugs 16, 779-786 (2002); and clinical experience: P. E. Keck Jr., S. L. McElroy, Expert Opin. Invest. Drugs 12, 655-662 (2003).