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

Queen Substance CAS Registry Number: 334-20-3 9-氧代-2-癸烯酸

CAS Name: (E)-9-Oxo-2-decenoic acid
Percent Composition: C 65.19%, H 8.75%, O 26.05%
Literature References: Secreted in the mandibular gland of queen honey bees (Apis mellifera, A. florea, A. cerana, A. dorsata); inhibits the development of ovaries in worker bees, prevents queen cell formation and attracts male bees (drones) to virgin queens for the purpose of mating: Butler, Experientia 13, 256 (1957); Sannasi, Rajulu, Life Sci. 10, part 2, 195 (1971). Similarity with the ovary inhibiting hormone of prawns (Leander serratus): Carlisle, Butler, Nature 177, 276 (1956). Extraction and purification: Carlisle, Butler, loc. cit.; Butler et al., Nature 184, 1871 (1959). Synthesis: Barbier et al., Compt. Rend. 251, 1133 (1960); Jaeger, Robinson, Tetrahedron 14, 320 (1961); Y. Naoshima et al., Agric. Biol. Chem. 48, 2151 (1984); U. P. Dhokte, A. S. Rao, Synth. Commun. 17, 355 (1987).

Lead Chromate(VI) Oxide CAS Registry Number: 18454-12-1 中国红,铬红

CAS Name: Chromic acid lead(2+) salt (1:2)
Additional Names: basic lead chromate; red lead chromate; chrome red; chromium lead oxide; Persian red; Austrian cinnabar
Percent Composition: Cr 9...
Literature References: See: Colour Index vol. 4, (3rd ed., 1971) p 4677.

Mosapride CAS Registry Number: 112885-41-3 莫沙必利

CAS Name: 4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]benzamide
Additional Names: (±)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methy...
Literature References: Selective 5-HT4 receptor agonist. Prepn: T. Kon et al., EP 243959; eidem, US 4870074 (1987, 1989 both to Dainippon); S. Kato et al., J. Med. Chem. 34, 616 (1991). Pharmacology: N. Yoshida et al., Arch. Int. Pharmacodyn. Ther. 300, 51 (1989). Series of articles on pharmacokinetics: Arzneim.-Forsch. 43, 859-872 (1993); on pharmacology and metabolism: ibid. 1083-1108. HPLC determn in plasma: I. Yokoyama et al., J. Pharm. Biomed. Anal. 15, 1527 (1997). Clinical evaluation in gastro-esphageal reflux disease: M. Ruth et al., Aliment. Pharmacol. Ther. 12, 35 (1998). Toxicity study: S. Yatera et al., Jpn. Pharmacol. Ther. 21, 21 (1993).

Piboserod CAS Registry Number: 152811-62-6 哌波色罗

CAS Name: N-[(1-Butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamidePercent Composition: C 71.51%, H 8.46%, N 11.37%, O 8.66%
Literature References: Selective 5-HT4 receptor antagonist. Prepn: L. M. Gaster, P. A. Wyman, WO 9318036; eidem, US 5852014 (1993, 1998 both to SKB). In vitro and in vivo studies of bioavailability, pharmacokinetics, and duration: K. A. Wardle et al., Br. J. Pharmacol. 118, 665 (1996). Effect on gastrointestinal function: G. J. Sanger et al., Neurogastroenterol. Motil. 10, 271 (1998); idem et al., Br. J. Pharmacol. 130, 706 (2000). Clinical evaluation in irritable bowel syndrome: L. A. Houghton et al., Aliment. Pharmacol. Ther. 13, 1437 (1999).

Lonapalene CAS Registry Number: 91431-42-4 氯萘帕林

CAS Name: 6-Chloro-2,3-dimethoxy-1,4-naphthalenediol diacetate
Additional Names: 6-chloro-1,4-diacetoxy-2,3-dimethoxynaphthalenePercent Composition: C 56.73%, H 4.46%, Cl 10.47%, O 28.34%
Literature References: Selective 5-lipoxygenase inhibitor. Prepn: G. H. Jones et al., EP 107512; eidem, US 4466981 (both 1984 to Syntex); eidem, J. Med. Chem. 29, 1504 (1986); S. T. Perri, H. W. Moore, Tetrahedron Lett. 28, 4507 (1987). Clinical pharmacology: A. K. Black et al., J. Invest. Dermatol. 95, 50 (1990). Percutaneous absorption and metabolism: P. A. Lehman et al., Pharm. Res. 9, 1145 (1992). HPLC determn in pharmaceutical prepns: R. A. Kenley et al., Drug Dev. Ind. Pharm. 11, 1781 (1985); of metabolites in urine: C.-H. Kiang, C. Lee, J. Chromatogr. 565, 339 (1991). Clinical evaluation in psoriasis: A. Lassus, S. Forsstrom, Br. J. Dermatol. 113, 103 (1985).

Doxazosin CAS Registry Number: 74191-85-8 多沙唑嗪

CAS Name: 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazine
Additional Names: 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimeth...
Literature References: Selective a1-adrenergic blocker related to prazosin, q.v. Prepn: S. F. Campbell, DE 2847623; idem, US 4188390 (1979, 1980 both to Pfizer). Cardiovascular pharmacology: P. B. Timmermans et al., Arch. Int. Pharmacodyn. Ther. 245, 218 (1980). HPLC determn in plasma: M. G. Cowlishaw, J. R. Sharman, J. Chromatogr. 344, 403 (1985). Clinical pharmacokinetics: H. L. Elliott et al., Br. J. Clin. Pharmacol. 13, 699 (1982). Symposia on pharmacology and clinical efficacy in hypertension: Br. J. Clin. Pharmacol. 21, Suppl. 1, 1S-92S (1986); Am. J. Cardiol. 59, 1G-104G (1987). Review of clinical trials in benign prostatic hypertrophy: C. G. Roehrborn, R. L. Siegel, Urology 48, 406-415 (1996).

Dimetofrine CAS Registry Number: 22950-29-4 二甲福林

CAS Name: 4-Hydroxy-3,5-dimethoxy-a-[(methylamino)methyl]benzenemethanol
Additional Names: 1-(3,5-dimethoxy-4-hydroxyphenyl)-2-(methylamino)ethanol; dimethophrine; dimetrophine
Percent Compo...
Literature References: Selective a1-adrenergic receptor agonist. Prepn: GB 1145637; M. Giani et al., US 3646144 (1969, 1972 both to Zambeletti). Pharmacology: Scrollini et al., Atti Accad. Med. Lomb. 25, 193, 203 (1970), C.A. 76, 54270a, 54425e (1972). Pharmacokinetics and metabolism: P. Boselli et al., Arzneim.-Forsch. 26, 2038 (1976); M. S. Benedetti et al., ibid. 27, 158 (1977). TLC determn: G. Musumarra et al., J. Chromatogr. 350, 151 (1985). Double blind clinical evaluations: V. Baldrighi et al., Curr. Med. Res. Opin. 9, 78 (1984); U. Marini et al., ibid. 265.

Galantamine CAS Registry Number: 357-70-0 加兰他敏

CAS Name: (4aS,6R,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-ol
Additional Names: galanthamine; lycoremine
Percent Composition: C 71.06%, H 7.3...
Literature References: Selective acetylcholinesterase inhibitor. Isoln from Caucasian snowdrops, Galanthus woronowii Vel., Amaryllidaceae: N. F. Proskurnina, A. P. Yakovleva, J. Gen. Chem. USSR 22, 1899 (1952); from Narcissus spp: Boit et al., Ber. 90, 725, 2197 (1957). Structure work: S. Kobayashi et al., Chem. Ind. (London) 1956, 177. Synthesis and stereochemistry: D. H. R. Barton, G. W. Kirby, Proc. Chem. Soc. London 1960, 392; eidem, J. Chem. Soc. 1962, 806. Asymmetric synthesis of isomers from L-tyrosine: K. Shimizu et al., Heterocycles 8, 277 (1977). Biosynthesis studies: D. H. R. Barton et al., J. Chem. Soc. 1963, 4545; W. Döbke, Heterocycles 6, 551 (1977). Toxicology study: S. L. Friess et al., Toxicol. Appl. Pharmacol. 3, 347 (1961). Clinical pharmacokinetics: U. Bickel et al., Clin. Pharmacol. Ther. 50, 420 (1991). Review of pharmacology: A. L. Harvey, Pharmacol. Ther. 68, 113-128 (1995); of clinical experience in Alzheimer's disease: R. Bullock, Exp. Rev. Neurother. 4, 153-163 (2004); of synthesis and pharmacology: J. Marco-Contelles et al., Chem. Rev. 106, 116-133 (2006).

Eplerenone CAS Registry Number: 107724-20-9 依普利酮

CAS Name: (7a,11a,17a)-9,11-Epoxy-17-hydroxy-3-oxopregn-4-ene-7,21-dicarboxylic acid g-lactone methyl ester
Additional Names: 9a,11-epoxy-7a-(methoxycarbonyl)-3-oxo-17a-pregn-4-ene-21,17-carbol...
Literature References: Selective aldosterone receptor antagonist (SARA); structurally similar to spironolactone, q.v. Prepn: J. Grob, J. Kalvoda, EP 122232; eidem, US 4559332 (1984, 1985 both to Ciba-Geigy); J. Grob et al., Helv. Chim. Acta 80, 566 (1997). Pharmacology and receptor binding studies: M. de Gasparo et al., J. Pharmacol. Exp. Ther. 240, 650 (1987). Clinical pharmacokinetics: W. R. Ravis et al., J. Clin. Pharmacol. 45, 810 (2005). Clinical trial in congestive heart failure after myocardial infarction: B. Pitt et al., N. Engl. J. Med. 348, 1309 (2003); in hypertension vs losartan: M. H. Weinberger et al., Am. Heart J. 150, 426 (2005). Review of pharmacology and clinical experience: J. A. Delyani et al., Cardiovasc. Drug Rev. 19, 185-200 (2001); E. Burgess, Expert Opin. Pharmacother. 5, 2573-2581 (2004).

Tasosartan CAS Registry Number: 145733-36-4 他索沙坦

CAS Name: 5,8-Dihydro-2,4-dimethyl-8-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]pyrido[2,3-d]pyrimidin-7(6H)-oneTrademarks: Verdia (Am. Home)
Percent Composition: C 67.14%, H 5.14%, N 2...
Literature References: Selective angiotensin II type 1 (AII1)-receptor antagonist. Prepn: J. W. Ellingboe et al., US 5149699 (1992 to Am. Home); idem et al., J. Med. Chem. 37, 542 (1994). Clinical tolerability in patients with essential hypertension: S. Oparil et al., Curr. Ther. Res. 58, 930 (1997); and efficacy: J. M. Neutel et al., Am. Heart J. 137, 118 (1999).