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

Mizolastine CAS Registry Number: 108612-45-9 咪唑斯汀

CAS Name: 2-[[1-[1-[(4-Fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(1H)-pyrimidinone
Additional Names: 2-[[1-[1-(p-fluorobenzyl)-2-benzimidazolyl]-4-piperidinyl]methy...
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: JP Kokai 87 61979; P. Manoury et al., US 4912219 (1987, 1990 both to Synthelabo). Receptor binding study: J. Benavides et al., Arzneim.-Forsch. 45, 551 (1995). HPLC determn in plasma: V. Ascalone et al., J. Chromatogr. 619, 275 (1993). Clinical pharmacokinetics: P. Rosenzweig et al., Ann. Allergy 69, 135 (1992). Effect on psychomotor performance: J. S. Kerr et al., Eur. J. Clin. Pharmacol. 47, 331 (1994). Clinical trial in allergic rhinitis: F. Leynadier et al., Ann. Allergy Asthma Immunol. 76, 163 (1996).

Terfenadine CAS Registry Number: 50679-08-8 特非那定

CAS Name: a-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol
Additional Names: 1-(p-tert-butylphenyl)-4-[4'-(a-hydroxydiphenylmethyl)-1'-piperidyl]butanol; a-(p-tert-...
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: A. A. Carr, C. R. Kinsolving, DE 2303306; eidem, US 3878217 (1973, 1975 both to Richardson-Merrell); A. A. Carr, D. R. Meyer, Arzneim.-Forsch. 32, 1157 (1982). Series of articles on chemistry, pharmacology, toxicology and clinical studies: ibid. 32, 1153-1218 (1982). Metabolism in human liver: M. Jurima-Romet et al., Drug Metab. Dispos. 22, 849 (1994). Comprehensive description: A. A. Badwan et al., Anal. Profiles Drug Subs. 19, 627-662 (1990). Review: H. C. Masheter, Clin. Rev. Allergy 11, 5-34 (1993).

Fexofenadine CAS Registry Number: 83799-24-0 非索芬那定

CAS Name: a,a-Dimethyl-4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]benzeneacetic acid
Additional Names: carboxyterfenadine; terfenadine carboxylatePercent Composition: C 76.61...
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: A.A. Carr et al., DE 3007498; eidem, US 4254129 (1980, 1981 both to Richardson-Merrell). Identification as active metabolite of terfenadine, q.v.: D. A. Garteiz et al., Arzneim.-Forsch. 32, 1185 (1982). Synthesis: S. H. Kawai et al., J. Org. Chem. 59, 2620 (1994). HPLC separation from terfenadine: K. Y. Chan et al., J. Chromatogr. 571, 291 (1991); determn in biological fluids: A. Terhechte, G. Blaschke, ibid. A 694, 219 (1995). Effects on cardiac K+ channels: D. Rampe et al., Mol. Pharmacol. 44, 1240 (1993). Comparative analysis of cardiotoxic potential: J. A. Hey et al., Arzneim.-Forsch. 46, 153 (1996). Clinical pharmacology in children: F. E. R. Simons et al., J. Allergy Clin. Immunol. 98, 1062 (1996).

Loratadine CAS Registry Number: 79794-75-5 氯雷他定

CAS Name: 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
Additional Names: 11-[N-(ethoxycarbonyl)-4-piperidylidene]-8-chloro-...
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: F. J. Villani, US 4282233 (1981 to Schering); F. J. Villani et al., Arzneim.-Forsch. 36, 1311 (1986). Pharmacology: A. Barnett et al., Agents Actions 14, 590 (1984). Evaluation of CNS effects in humans: C. M. Bradley, A. N. Nicholson, Eur. J. Clin. Pharmacol. 32, 419 (1987). Clinical pharmacokinetics: E. Radwanski et al., J. Clin. Pharmacol. 27, 530 (1987). Clinical trial in allergic rhinitis: R. J. Dockhorn et al., Ann. Allergy 58, 407 (1987); in comparison with terfenadine, q.v.: F. Horak et al., Arzneim.-Forsch. 38, 124 (1988); G. Bruttmann et al., J. Allergy Clin. Immunol. 83, 411 (1989). HPLC determn in plasma: O. Q. P. Yin et al., J. Chromatogr. B 796, 165 (2003). Review of pharmacology and therapeutic efficacy: M. Haria et al., Drugs 48, 617-637 (1994).

Astemizole CAS Registry Number: 68844-77-9 阿司咪唑

CAS Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
Additional Names: 1-(p-fluorobenzyl)-2-[[1-(p-methoxyphenethyl)-4-piperidyl]amino]ben...
Literature References: Nonsedating-type histamine H1-receptor antagonist. Prepn: F. Janssens et al., EP 5318; eidem, US 4219559 (1979, 1980 both to Janssen). Pharmacology: J. Van Wauwe et al., Arch. Int. Pharmacodyn. Ther. 251, 39 (1981); A. Wauquier, C. J. E. Niemegeers, Eur. J. Pharmacol. 72, 245 (1981). In vitro and in vivo binding characteristics: P. M. Laduron et al., Mol. Pharmacol. 21, 294 (1982). Effect on human psychomotor performance: T. Seppala, K. Savolainen, Curr. Ther. Res. 31, 638 (1982). Clinical study in treatment of hay fever: J. Callier et al., ibid. 29, 24 (1981). Mutagenicity study: P. Vanparys et al., Arch. Toxicol. 50, 167 (1982). Review of pharmacology and clinical trials: D. M. Richards et al., Drugs 28, 38-61 (1984). Comprehensive description: A. M. Al-Obaid, M. S. Mian, Anal. Profiles Drug Subs. 20, 173-208 (1991).

Desloratadine CAS Registry Number: 100643-71-8 地氯雷他定

CAS Name: 8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Additional Names: descarboethoxyloratadineTrademarks: Clarinex (Schering-Plough)
Percent Compos...
Literature References: Nonsedating-type histamine H1-receptor antagonist; active metabolite of loratadine, q.v. Also inhibits generation and release of inflammatory mediators from basophils and mast cells. Prepn: D. P. Schumacher et al., EP 208855; F. J. Villani, J. K. Wong, US 4659716 (both 1987 to Schering). GLC determn in plasma: R. Johnson et al., J. Chromatogr. B 657, 125 (1994). Pharmacology: W. Kreutner et al., Arzneim.-Forsch. 50, 345 (2000). Series of articles on clinical efficacy in rhinitis, asthma and urticaria: Allergy 56, Suppl. 65, 1-32 (2001). Review of pharmacology, pharmacokinetics and clinical efficacy: R. S. Geha, E. O. Meltzer, J. Allergy Clin. Immunol. 107, 751-762 (2001); D. K. Agrawal, Expert Opin. Invest. Drugs 10, 547-560 (2001).

Carvedilol CAS Registry Number: 72956-09-3 卡维地洛

CAS Name: 1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanolTrademarks: Coreg (GSK); Dilatrend (Roche); Dimitone (Erco); Eucardic (Roche); Kredex (GSK); Querto (Byk Gulden) Literature References: Nonselective b-adrenergic blocker with a1-blocking activity. Prepn: F. Wiedemann et al., DE 2815926; eidem, US 4503067 (1979, 1985 both to Boehringer Mannheim). General pharmacological profile: M. Hirohashi et al., Arzneim.-Forsch. 40, 735 (1990). HPLC determn in biological fluids: K. Reiff, J. Chromatogr. 413, 355 (1987). Series of articles on clinical pharmacology and efficacy in hypertension: J. Cardiovasc. Pharmacol. 19, Suppl. 1, S1-S146 (1992). Clinical trial in chronic heart failure: M. Packer et al., N. Engl. J. Med. 334, 1349 (1996). Review: W. H. Frishman, ibid. 339, 1759-1765 (1998).

Bucindolol CAS Registry Number: 71119-11-4 布新洛尔

CAS Name: 2-[2-Hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy]benzonitrile
Percent Composition: C 72.70%, H 6.93%, N 11.56%, O 8.80%
Literature References: Non-selective b-adrenergic blocker with vasodilating activity. Prepn: BE 868943 (1979 to Bristol-Myers); W. E. Kreighbaum, W. T. Comer, US 4234595 (1980 to Mead Johnson); W. E. Kreighbaum et al., J. Med. Chem. 23, 285 (1980). Crystal structure: J.-M. Léger et al., Acta Crystallogr. C40, 706 (1984). Conformation: E. Coutinho, Indian J. Chem. 34B, 553 (1995). Review of chemistry and pharmacology: D. Deitchman et al., in New Drugs Annual: Cardiovascular Drugs vol. 1, A. Scriabine, Ed. (Raven Press, New York, 1983) pp 1-18. Clinical pharmacokinetics: P. A. Meredith et al, Xenobiotica 15, 979 (1985). Clinical pharmacology: N. Bett et al., Am. J. Cardiol. 57, 678 (1986). GC-MS determn in plasma: M. J. Bartek et al., J. Chromatogr. 377, 183 (1986). Evaluation in congestive heart failure: M. R. Bristow et al., Circulation 89, 1632 (1994).

Tertatolol CAS Registry Number: 34784-64-0 特他洛尔

CAS Name: 1-[(3,4-Dihydro-2H-1-benzothiopyran-8-yl)oxy]-3-[(1,1-dimethylethyl)amino]-2-propanol
Additional Names: (±)-1-tert-butylamino-3-(1-thiachroman-8-yloxy)-2-propanol; dl-8-[2-hydrox...
Literature References: Nonselective b-adrenergic blocker. Prepn: C. Malen, M. Laubie, DE 2115201; eidem, US 3960891 (1971, 1976 both to Sci. Union et Cie). Pharmacology in animals: M. Laubie et al., Arch. Int. Pharmacodyn. Ther. 201, 323, 334 (1973); B. R. Walker et al., J. Cardiovasc. Pharmacol. 7, 1193 (1985). Synergistic effect with indapamide, q.v.: E. Marmo et al., Drugs Exp. Clin. Res. 11, 709 (1985). GC-MS determn in plasma and urine: S. Staveris et al., J. Chromatogr. 339, 97 (1985). Pharmacology in humans and mechanism of action study: A. De Blasi et al., Clin. Pharmacol. Ther. 39, 245 (1986). Preliminary evaluation in hypertension: J. P. Degaute et al., Am. J. Hypertens. 1, 263S (1988).

Bopindolol CAS Registry Number: 62658-63-3 波吲洛尔

CAS Name: 1-[(1,1-Dimethylethyl)amino]-3-[(2-methyl-1H-indol-4-yl)oxy]-2-propanol benzoate ester
Additional Names: (±)-1-(tert-butylamino)-3-[(2-methylindol-4-yl)oxy]-2-propanol benzoate (...
Literature References: Nonselective b-adrenergic blocker. Prepn: F. Troxler, F. Seemann, DE 2635209; eidem, US 4340541 (1977, 1982 both to Sandoz). Clinical pharmacology: P. van Brummelen et al., Eur. J. Clin. Pharmacol. 22, 491 (1982). HPLC determn in plasma: C. J. Oddie et al., J. Chromatogr. 273, 469 (1983). Effect on plasma lipid fractions: P. van Brummelen et al., Br. J. Clin. Pharmacol. 17, 86 (1984). Pharmacokinetics: R. Platzer et al., Clin. Pharmacol. Ther. 36, 5 (1984). Clinical trials in hypertension: U. L. Hulthen et al., J. Cardiovasc. Pharmacol. 5, 426 (1983); W. J. Schiess et al., Eur. J. Clin. Pharmacol. 27, 529 (1984).