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

Phenazopyridine CAS Registry Number: 94-78-0 非那吡啶

CAS Name: 3-(Phenylazo)-2,6-pyridinediamine
Additional Names: 2,6-diamino-3-phenylazopyridine; b-phenylazo-a,a'-diaminopyridine
Percent Composition: C 61.96%, H 5.20%, N 32.84%
Literature References: Azo dye used in treatment of urinary tract infections. Prepn: A. E. Chichibabin, O. A. Zeide, J. Russ. Phys. Chem. Soc. 46, 1216 (1914); Chem. Zentralbl. 1915, I, 1064; I. Ostromislensky, US 1680109 (1928 to Pyridium); and bacteriostatic properties: R. N. Shreve et al., J. Am. Chem. Soc. 65, 2241 (1943). Physical characteristics: G. W. Collins, J. Am. Pharm. Assoc. 20, 455 (1931). Toxicity data: B. A. Becker, J. G. Swift, Toxicol. Appl. Pharmacol. 1, 42 (1959). Comprehensive description: K. W. Blessel et al., Anal. Profiles Drug Subs. 3, 465-482 (1974). LC-MS determn in plasma and pharmacokinetics: E. Shang et al., Anal. Bioanal. Chem. 382, 216 (2005). Review of clinical experience in urinary tract infections: S. A. Zelenitsky, G. G. Zhanel, Ann. Pharmacother. 30, 866-868 (1996).

Dobutamine CAS Registry Number: 34368-04-2 多巴酚丁胺

CAS Name: 4-[2-[[3-(4-Hydroxyphenyl)-1-methylpropyl]amino]ethyl]-1,2-benzenediol
Additional Names: (±)-4-[2-[[3-(p-hydroxyphenyl)-1-methylpropyl]amino]ethyl]pyrocatechol; 3,4-dihydroxy-N-[...
Literature References: b1-Adrenergic agonist; derivative of dopamine, q.v. Prepn: R. R. Tuttle, J. Mills, DE 2317710; eidem, US 3987200 (1973, 1976 to Lilly). Pharmacology: R. Weber, R. R. Tuttle in Pharmacological and Biochemical Properties of Drug Substances vol. 1, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1977) pp 109-124; E. H. Sonnenblick et al., N. Engl. J. Med. 300, 17 (1979). Comprehensive description: R. H. Bishara, H. B. Long, Anal. Profiles Drug Subs. 8, 139-158 (1979).

Metoprolol CAS Registry Number: 37350-58-6

CAS Name: 1-[4-(2-Methoxyethyl)phenoxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-(isopropylamino)-3-[p-(b-methoxyethyl)phenoxy]-2-propanolPercent Composition: C 67.38%, ...
Literature References: b1-Adrenergic blocker lacking intrinsic sympathomimetic activity. Prepn: A. E. Brandstrom et al., DE 2106209; eidem, US 3998790 (1971, 1976 both to AB Hässle). Pharmacology: B. Ablad et al., Life Sci. 12, 107 (1973); Johansson, Eur. J. Pharmacol. 24, 194 (1973). Toxicology: N.-O. Bodin et al., Acta Pharmacol. Toxicol. 36, Suppl. V, 96 (1975). Clinical trials in acute myocardial infarction: L. Rydén et al., N. Engl. J. Med. 308, 614 (1983); Drugs 29, Suppl. 1, 2-8 (1985); in chronic heart failure: A. Hjalmarson et al., J. Am. Med. Assoc. 283, 1295 (2000). Comprehensive description: J. R. Luch, Anal. Profiles Drug Subs. 12, 325-356 (1983). Review of pharmacology, therapeutic efficacy: P. Benfield et al., Drugs 31, 376-429 (1986).

Xamoterol CAS Registry Number: 81801-12-9 扎莫特罗

CAS Name: N-[2-[[2-Hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide
Additional Names: 1-(4-hydroxyphenoxy)-3-[2-(4-morpholinocarboxamido)ethylamino]-2-propanol
Percent...
Literature References: b1-Adrenoceptor partial agonist. Prepn: BE 867376; B. G. Main, J. J. Barlow, US 4143140 (1978, 1979 both to ICI); prepn and adrenoceptor stimulant activity: J. J. Barlow et al., J. Med. Chem. 24, 315 (1981). Cardiovascular activity: A. Nuttall, H. M. Snow, Br. J. Pharmacol. 77, 381 (1982). Hemodynamics, cardioselectivity and kinetics: G. Jennings et al., Clin. Pharmacol. Ther. 35, 594 (1984). Hemodynamic effects: J.-M. R. Detry et al., Eur. Heart J. 4, 584 (1983); H. Sato et al., Circulation 75, 213 (1987). Metabolism: T. R. Marten et al., Drug Metab. Dispos. 12, 652 (1984). HPLC determn in biological fluids: C. J. Oddie et al., J. Chromatogr. 308, 370 (1984). Clinical evaluations: F. L. Tseu et al., Br. Heart J. 56, 469 (1986); L. Barrios et al., Eur. J. Clin. Pharmacol. 29, 667 (1986). Clinical comparison with atenolol, q.v., in asthmatic patients: J. W. J. Lammers et al., Br. J. Clin. Pharmacol. 22, 595 (1986).

Fenoterol CAS Registry Number: 13392-18-2 非诺特罗

CAS Name: 5-[1-Hydroxy-2-[[2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-1,3-benzenediol
Additional Names: 3,5-dihydroxy-a-[[(p-hydroxy-a-methylphenethyl)amino]methyl]benzyl alcohol; 1-(3,5-di...
Literature References: b2-Adrenergic agonist. Prepn and sepn of stereoisomers: BE 640433; Zelle et al., US 3341593 (1962, 1967 to Boehringer, Ing.). Pharmacology: Schuster, Baum, Arzneim.-Forsch. 19, 1905 (1969); O'Donnell, Eur. J. Pharmacol. 12, 35 (1970). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Metabolism in mice: S. Kojima et al., Arzneim.-Forsch. 30, 959 (1980). HPLC determn in plasma: S. Kramer, G. Blaschke, J. Chromatogr. B 751, 169 (2001). Clinical evaluation: Tweel, Ann. Allergy 29, 142 (1971); Rebuck, Saunders, Med. J. Aust. 1, 225 (1972). Comparison with ritodrine in preterm labor: J. Gerris et al., Eur. J. Clin. Pharmacol. 18, 443 (1980). Review of pharmacology and therapeutic efficacy: R. C. Heel et al., Drugs 15, 3-32 (1978); N. Svedmyr, Pharmacotherapy 5, 109-126 (1985).

Hexoprenaline CAS Registry Number: 3215-70-1 海索那林

CAS Name: 4,4'-[1,6-Hexanediylbis[imino(1-hydroxy-2,1-ethanediyl)]]bis-1,2-benzenediol
Additional Names: a,a'-[hexamethylenebis(iminomethylene)]bis[3,4-dihydroxybenzyl alcohol]; N,N'-bis[2-(3,4...
Literature References: b2-Adrenergic agonist. Prepn: O. Schmid et al., AT 241436; eidem, US 3329709 (1965, 1967, both to OSSW); Schmid et al., DE 1215729 (1966 to Lentia GmbH). Pharmacology: Thiede et al., Arzneim.-Forsch. 21, 416 (1971). Clinical studies: Schindl, ibid. 20, 1755 (1970); several authors in Wien. Klin. Wochenschr. 83, 75, 80, 101, 114, 117, 130 (1971). Clinical evaluation for interruption of labor: J. Lipshitz et al., J. Reprod. Med. 31, 1023 (1986).

Bitolterol CAS Registry Number: 30392-40-6 比托特罗

CAS Name: 4-Methylbenzoic acid 4-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-1,2-phenylene ester
Additional Names: p-toluic acid 4-[2-(t-butylamino)-1-hydroxethyl]-o-phenylene ester; a-[(tert...
Literature References: b2-Adrenergic agonist; a diester of N-tert-butylnorepinephrine. Prepn: H. Minatoya et al., DE 2015573; eidem, US 4138581 (1970, 1979 both to Sterling); B. F. Tullar et al., J. Med. Chem. 19, 834 (1976). Pharmacology: H. Minatoya, J. Pharmacol. Exp. Ther. 206, 515 (1978). Metabolism and excretion: T. Aimoto et al., Xenobiotica 9, 173 (1979). Comparative clinical studies with isoproterenol, q.v., in asthma: J. L. Pinnas et al., J. Allergy Clin. Immunol. 79, 768 (1987); R. A. Nathan et al., ibid. 822. Review: S. B. Walker et al., Pharmacotherapy 5, 127-137 (1985).

Salmeterol CAS Registry Number: 89365-50-4 沙美特罗

CAS Name: 4-Hydroxy-a1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol
Additional Names: (±)-4-hydroxy-a1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-m-xylene-a,a1-diolPercent ...
Literature References: b2-Adrenergic agonist; structural analog of albuterol, q.v. Prepn: I. F. Skidmore et al., DE 3414752; eidem, US 4992474 (1984, 1991 both to Glaxo). Pharmacology: M. Johnson, Lung 168, Suppl., 115 (1990). Preliminary evaluations in asthma: A. Ullman et al., Am. Rev. Respir. Dis. 142, 571 (1990); O. P. Twentyman et al., Lancet 336, 1338 (1990). Review of pharmacology and therapeutic use: R. N. Brogden, D. Faulds, Drugs 42, 895-912 (1991).

Cimaterol CAS Registry Number: 54239-37-1 西马特罗

CAS Name: 2-Amino-5-[1-hydroxy-2-[(1-methylethyl)amino]ethyl]benzonitrile
Additional Names: (±)-5-[1-hydroxy-2-(isopropylamino)ethyl]anthranilonitrile; 1-(4-amino-3-cyanophenyl)-2-isopropy...
Literature References: b-Adrenergic agonist, related to clenbuterol and mabuterol, q.q.v. Prepn: G. Engelhardt et al., DE 2261914 (1974 to Thomae). Pharmacology: G. Engelhardt, Arzneim.-Forsch. 34, 1625 (1984). Effect on lipid metabolism in sheep: C. Y. Hu et al., J. Anim. Sci. 66, 1393 (1988). Efficacy as a repartitioning agent in livestock: R. W. Jones et al., ibid. 61, 905 (1985); D. H. Beermann et al., ibid. 62, 370 (1986). Review: M. Lafontan et al., Reprod. Nutr. Dev. 28, 61-84 (1988).

Isoproterenol CAS Registry Number: 7683-59-2 异丙肾上腺素

CAS Name: 4-[1-Hydroxy-2-[(1-methylethyl)amino]ethyl]-1,2-benzenediol
Additional Names: 3,4-dihydroxy-a-[(isopropylamino)methyl]benzyl alcohol; a-(isopropylaminomethyl)protocatechuyl alcohol; i...
Literature References: b-Adrenergic agonist. Catecholamine derivative prepd by the reaction of 3,4-dihydroxy-a-haloacetophenone with an excess of isopropylamine: Scheuing, Thomä, DE 723278 (1942 to Boehringer, Ing.); US 2308232 (1943); from guaiacol and chloral hydrate: Beke et al., Pharm. Zentralhalle 92, 237 (1953). Resolution: Kerschbaum, Benedikt, Monatsh. Chem. 83, 1090 (1952); Beccari et al., Science 118, 249 (1953); Delmar et al., US 2715141 (1955 to Delmar Chem.). Configuration: Pratesi et al., Farmaco Ed. Sci. 15, 3 (1960). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Effect on gastric acid secretion: M. J. Daly, Scand. J. Gastroenterol. 89, 3 (1984). Use in treatment of primary pulmonary hypertension: D. A. Pietro et al., N. Engl. J. Med. 310, 1032 (1984). Review of pharmacology and comparison with other b-adrenoceptor agonists: V. T. Popa, J. Asthma 21, 183-207 (1984). Comprehensive description: M. Tariq, A. A. Al-Badr, Anal. Profiles Drug Subs. 14, 391-422 (1985).