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

Epanolol CAS Registry Number: 86880-51-5 依泮洛尔

CAS Name: N-[2-[[3-(2-Cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-4-hydroxybenzeneacetamide
Additional Names: 1-(2-cyanophenoxy)-3-b-(4-hydroxyphenylacetamido)ethylamino-2-propanolPercent Compos...
Literature References: Cardio-selective b1-adrenergic blocker with intrinsic sympathomimetic activity. Prepn: L. H. Smith, DE 2362568; idem, US 4167581 (1974, 1979 both to ICI). Clinical pharmacology: T. H. Pringle et al., Br. J. Clin. Pharmacol. 21, 249 (1986). Clinical pharmacokinetics: I. D. Cockshott et al., Biopharm. Drug Dispos. 11, 253 (1990). Clinical evaluation in hypertension: B. Dahlof et al., Br. J. Clin. Pharmacol. 18, 831 (1984); in angina: J. Boberg et al., Clin. Cardiol. 15, 591 (1992).

Cetamolol CAS Registry Number: 34919-98-7 塞他洛尔

CAS Name: 2-[2-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]phenoxy]-N-methylacetamide
Additional Names: 2-[o-[3-(t-butylamino)-2-hydroxypropoxy]phenoxy]-N-methylacetamide; (±)-1-t-butyl...
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 767781; D. J. Lecount, C. J. Squire, US 4059622 (1971, 1977 both to ICI). Cardiovascular effects in dogs: G. Beaulieu et al., Can. J. Physiol. Pharmacol. 63, 610 (1984). Determn in human serum: M. D. Stern, Clin. Biochem. 17, 162 (1984). Pharmacology and pharmacodynamics in humans: M. A. Klausner et al., Curr. Ther. Res. 36, 379 (1984); J. Coelho et al., Br. J. Clin. Pharmacol. 19, 411 (1985). Evaluation in hypertensive patients: W. B. White et al., Clin. Pharmacol. Ther. 39, 664 (1986).

Bevantolol CAS Registry Number: 59170-23-9 贝凡洛尔

CAS Name: 1-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol
Additional Names: 1-[(3,4-dimethoxyphenethyl)amino]-3-(m-tolyloxy)-2-propanol
Percent Composition: C 69.54%, ...
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 790165; A. Holmes, R. F. Meyer, US 3857891 (1973, 1974 both to Parke, Davis Co.); M. L. Hoefle et al., J. Med. Chem. 18, 148 (1975). Pharmacology in animals: S. G. Hastings et al., Arch. Int. Pharmacodyn. Ther. 226, 81 (1977). Cardiovascular effects in animals: I. D. Dukes, E. M. Vaughan Williams, Br. J. Pharmacol. 84, 365 (1985). Cardioselectivity in asthmatic patients: C.-G. Löfdahl et al., Pharmacotherapy 4, 205 (1984). GC determn in plasma: E. J. Randinitis et al., J. Chromatogr. 308, 345 (1984). Pharmacokinetics in humans: P. Vermeij, P. van Brummelen, Eur. J. Clin. Pharmacol. 30, 375 (1986). Comparative clinical trial with hydrochlorothiazide in hypertension: C. P. Lucas et al., Clin. Ther. 8, 49 (1985). Symposium on pharmacology and clinical efficacy: Am. J. Cardiol. 58, 1E-44E (1986).

Celiprolol CAS Registry Number: 56980-93-9 塞利洛尔

CAS Name: N'-[3-Acetyl-4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-N,N-diethylurea
Additional Names: N-[3-acetyl-4-(3'-tert-butylamino-2'-hydroxy)propoxy]phenyl-N'-diethylureaPerce...
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 823411; G. Zölss et al., US 4034009 (1975, 1977 both to Chemie Linz). Hemodynamic effects: J. Bonelli et al., Wien. Klin. Wochenschr. 90, 350 (1978); H. Pittner, Arch. Pharmacol. 311, Suppl., 180 (1980). Series of articles on determn in biological material, pharmacology, toxicology, clinical studies: Arzneim.-Forsch. 33, 1-79 (1983). Toxicity: W. Wendtlandt, H. Pittner, ibid. 41. Symposium on pharmacology, clinical efficacy and comparison with other b-blockers: J. Cardiovasc. Pharmacol. 8, Suppl. 4, S1-S152 (1986). Comprehensive description: D. J. Mazzo et al., Anal. Profiles Drug Subs. 20, 237-301 (1991).

Bisoprolol CAS Registry Number: 66722-44-9 比索洛尔

CAS Name: 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-[[a-(2-isopropoxyethoxy)-p-tolyl]oxy]-3-(isopropylamino)-2-propanol; (...
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 859425; R. Jonas et al., US 4258062 (1978, 1981 both to E. Merck). Clinical pharmacology: A. E. Tattersfield et al., Br. J. Clin. Pharmacol. 18, 343 (1984); P. Dorow, U. Tönnesmann, Eur. J. Clin. Pharmacol. 27, 135 (1984). Binding study of (-)-form: A. J. Kaumann, H. Lemoine, Arch. Pharmacol. 331, 27 (1985). HPLC determn of enantiomers in plasma and urine: T. Suzuki et al., J. Chromatogr. 619, 267 (1993). Clinical evaluation in angina: R. S. Kohli et al., Eur. Heart J. 6, 845 (1985); in hypertension: F. R. Bühler et al., J. Cardiovasc. Pharmacol. 8, Suppl. 11, S122 (1986). Review of pharmacokinetics: J. Grevel et al., Clin. Pharmacokinet. 17, 53-63 (1989); of clinical efficacy in combination with hydrochlorothiazide: P. K. Zachariah et al., Clin. Ther. 15, 779-787 (1993). Clinical trial in chronic heart failure: CIBIS-II Investigators, Lancet 353, 9 (1999).

Betaxolol CAS Registry Number: 63659-18-7 倍他洛尔

CAS Name: 1-[4-[2-(Cyclopropylmethoxy)ethyl]-phenoxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
Perc...
Literature References: Cardioselective b1-adrenergic blocker. Prepn: P. M. J. Manoury et al., DE 2649605; eidem, US 4252984 (1977, 1981 both to Synthelabo). Blood concn and pharmacodynamic effects: S. J. Warrington et al., Br. J. Clin. Pharmacol. 10, 449 (1980). Pharmacokinetics: G. Bianchetti et al., Arzneim.-Forsch. 30, 1912 (1980). Cardiovascular effects in normal volunteers: P. J. Cadigan et al., Br. J. Clin. Pharmacol. 9, 569 (1980). Efficacy and pharmacokinetics: K. Balnave et al., ibid. 11, 171 (1981). Use in treatment of glaucoma: A. R. Berrospi, H. M. Leibowitz, Arch. Ophthalmol. 100, 943 (1982). Antihypertensive effect: M. Pathe et al., Therapie 37, 75 (1982). Book: Betaxolol and Other b1-Adrenoceptor Antagonists, P. L. Morselli et al., Eds. (Raven Press, New York, 1983) 385 pp.

Atenolol CAS Registry Number: 29122-68-7 阿替洛尔

CAS Name: 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzeneacetamide
Additional Names: 2-[p-[2-hydroxy-3-(isopropylamino)propoxy]phenyl]acetamide; 1-p-carbamoylmethylphenoxy-3-isopropylamino...
Literature References: Cardioselective b-adrenergic blocker. Prepn: Barrett et al., DE 2007751; eidem, US 3663607 and US 3836671 (1970, 1972, 1974 all to I.C.I.). Pharmacology and clinical studies: Giudicelli et al., C.R. Seances Soc. Biol. Ses Fil. 167, 232 (1973); Hansson et al., Acta Med. Scand. 194, 549 (1973); Amery et al., N. Engl. J. Med. 290, 284 (1974). Clinical trial in treatment of alcohol withdrawal syndrome: M. L. Kraus et al., ibid. 313, 905 (1985). HPLC determn of enantiomers in plasma and urine: S. K. Chin et al., J. Chromatogr. 489, 438 (1989). Comprehensive description: V. Caplar et al., Anal. Profiles Drug Subs. 13, 1-25 (1984). Review: J. D. Fitzgerald in Pharmacological and Biochemical Properties of Drug Substances vol. 2, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1979) pp 98-147; E. Marmo, Drugs Exp. Clin. Res. 6, 639-663 (1980). Symposium on clinical studies: Drugs 25, Suppl. 2, 1-346 (1983).

Esmolol CAS Registry Number: 81147-92-4 盐酸艾司洛尔

CAS Name: 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzenepropanoic acid methyl ester
Additional Names: (±)-methyl 3-[4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl]propionate; methyl p...
Literature References: Cardioselective b-adrenergic blocker. Prepn: E. I. Carlsson et al., EP 41491 (1982 to A.B. Hässle), C.A. 96, 122391f (1982); P. W. Erhardt et al., EP 53435; eidem, US 4593119 (1982, 1986 both to Am. Hosp. Supply); P. W. Erhardt et al., J. Med. Chem. 25, 1408 (1982). Pharmacology: R. J. Gorczynski et al., J. Cardiovasc. Pharmacol. 5, 668 (1983); eidem, ibid. 6, 1548 (1984). Pharmacokinetics: A. Yacobi et al., J. Pharm. Sci. 72, 711 (1983). GC-MS determn in blood: C. Y. Sum, A. Yacobi, ibid. 73, 1177 (1984). Clinical studies of effect in supraventricular tachycardia: G. Klein et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 22, 112 (1984); R. J. Gray et al., J. Am. Coll. Cardiol. 5, 1451 (1985). Symposium on pharmacology and clinical efficacy: Am. J. Cardiol. 56(11), 1F-62F (1985). Review of pharmacology and clinical efficacy: P. Benfield, E. M. Sorkin, Drugs 33, 392-412 (1987).

Acebutolol CAS Registry Number: 37517-30-9 醋丁洛尔

CAS Name: N-[3-Acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]butanamide
Additional Names: 3'-acetyl-4'-[2-hydroxy-3-(isopropylamino)propoxy]butyranilide; 1-(2-acetyl-4-n-butyramido...
Literature References: Cardioselective b-adrenergic blocker. Prepn: K. R. H. Wooldridge, B. Basil, ZA 6808345; eidem, US 3857952 (1969, 1974 both to May Baker). Pharmacology: Cuthbert, Owusu-Ankomah, Br. J. Pharmacol. 43, 639 (1971); Basil et al., ibid. 48, 198 (1973); Lewis et al., Br. Heart J. 35, 743 (1973). HPLC determn in plasma and urine: M. Piquette-Miller et al., J. Chromatogr. 526, 129 (1990). Crystal structure: A. Carpy et al., Acta Crystallogr. B35, 185 (1979). Review of pharmacology and therapeutic efficacy: B. N. Singh et al., Drugs 29, 531-569 (1985); G. DeBono et al., Am. Heart J. 109, 1211-1223 (1985). Comprehensive description: R. T. Foster, R. A. Carr, Anal. Profiles Drug Subs. 19, 1-26 (1990).

Landiolol CAS Registry Number: 133242-30-5 兰地洛尔

CAS Name: 4-[(2S)-2-Hydroxy-3-[[2-[(4-morpholinylcarbonyl)amino]ethyl]amino]propoxy]benzenepropanoic acid [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl ester
Additional Names: (-)-2,2-dimethyl-1,...
Literature References: Cardioselective b-adrenergic blocker. Prepn: S. Iguchi et al., EP 397031; US 5013734 (1990, 1991 both to Ono Pharm.); idem et al., Chem. Pharm. Bull. 40, 462 (1992). Electrophysiology: A. Sugiyama et al., J. Cardiovasc. Pharmacol. 34, 70 (1999). Clinical pharmacology: A. Kitamura et al., Eur. J. Clin. Pharmacol. 51, 467 (1997). Clinical pharmacokinetics in patients with cardiac tachyarrhythmias: H. Atarashi et al., Clin. Pharmacol. Ther. 68, 143 (2000).