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

Rofecoxib CAS Registry Number: 162011-90-7 罗非昔布

CAS Name: 4-[4-(Methylsulfonyl)phenyl]-3-phenyl-2(5H)-furanoneTrademarks: Vioxx (Merck Co.)
Percent Composition: C 64.95%, H 4.49%, O 20.36%, S 10.20%
Literature References: Selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: Y. Ducharme et al., WO 9500501; eidem, US 5474995 (both 1995 to Merck Frosst). HPLC determn in plasma: C. M. Chavez-Eng et al., J. Chromatogr. B 748, 31 (2000). Enzyme inhibition and clinical evaluation in dental pain: E. W. Ehrich et al., Clin. Pharmacol. Ther. 65, 336 (1999). Evaluation of risk of gastrointestinal effects in patients with osteoarthritis: M. J. Langman et al., J. Am. Med. Assoc. 282, 1929 (1999); with rheumatoid arthritis: C. Bombardier et al., N. Engl. J. Med. 343, 1520 (2000). Review of pharmacology and clinical experience: A. J. Matheson, D. P. Figgitt, Drugs 61, 833-865 (2001).

Montelukast CAS Registry Number: 158966-92-8 孟鲁司特

CAS Name: 1-[[[(1R)-1-[3-[(1E)-2-(7-Chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid
Percent Composition: C 71.71%, H 6.19%, C...
Literature References: Selective cysteinyl leukotriene type 1 receptor antagonist. Prepn: M. L. Belley et al., EP 480717; eidem, US 5565473 (1992, 1996 both to Merck Frosst); M. Labelle et al., Bioorg. Med. Chem. Lett. 5, 283 (1995). Pharmacological profile: T. R. Jones et al., Can. J. Physiol. Pharmacol. 73, 191 (1995). LC determn in human plasma: R. D. Amin et al., J. Pharm. Biomed. Anal. 13, 155 (1995). Review of pharmacology and clinical efficacy in asthma: A. Markham, D. Faulds, Drugs 56, 251-256 (1998). Clinical trial in pediatric asthma: B. Knorr et al., J. Am. Med. Assoc. 279, 1181 (1998); with loratadine, q.v., in allergic rhinitis: E. O. Meltzer et al., J. Allergy Clin. Immunol. 105, 917 (2000). Comparison with cetirizine, q.v., in urticaria: M. L. Pacor et al., Clin. Exp. Allergy 31, 1607 (2001). Review of pharmacology and clinical experience: Z. Diamant, A. P. Sampson, J. Drug Eval. Respir. Med. 1, 53-88 (2002).

Nemonapride CAS Registry Number: 75272-39-8 奈莫必利

CAS Name: rel-5-Chloro-2-methoxy-4-(methylamino)-N-[(2R,3R)-2-methyl-2-(phenylmethyl)-3-pyrrolidinyl]benzamide
Additional Names: (±)-cis-N-(1-benzyl-2-methyl-3-pyrrolidinyl)-5-chloro-4-(me...
Literature References: Selective dopamine D2 receptor antagonist. Prepn: M. Takashima et al., JP Kokai 79 14965; eidem, US 4210660 (1979, 1980 both to Yamanouchi); S. Iwanami et al., J. Med. Chem. 24, 1224 (1981). Pharmacology: M. Yamamoto et al., Neuropharmacology 21, 945 (1982). Dopamine receptor binding study: C. W. Grewe et al., Eur. J. Pharmacol. 81, 149 (1982). Use as a label for D2 receptors: A. S. Unis et al., Life Sci. 47, PL151 (1990). HPLC determn in plasma: T. Nagasaki et al., J. Chromatogr. B 714, 293 (1998). Clinical evaluation in schizophrenia: K. Satoh et al., Int. Clin. Psychopharmacol. 11, 279 (1996).

Ropinirole CAS Registry Number: 91374-21-9 罗匹尼罗

CAS Name: 4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one
Additional Names: 4-[2-(di-n-propylamino)ethyl]-2(3H)-indolonePercent Composition: C 73.81%, H 9.29%, N 10.76%, O 6.14%
Literature References: Selective dopamine D2-receptor agonist. Prepn: G. Gallagher, Jr., US 4452808 (1984 to Smithkline Beckman); idem et al., J. Med. Chem. 28, 1533 (1985). HPLC determn in plasma: J. E. Swagzdis, B. A. Mico, J. Pharm. Sci. 75, 90 (1986). Pharmacology and receptor binding study: R. J. Eden et al., Pharmacol. Biochem. Behav. 38, 147 (1991). Clinical pharmacology, pharmacokinetics: C. de Mey et al., Br. J. Clin. Pharmacol. 32, 483 (1991). Clinical trials in Parkinson's disease: O. Rascol et al., Mov. Disord. 13, 39 (1998); A. D. Korczyn et al., ibid. 46; in restless legs syndrome: A. S. Walters et al., ibid. 19, 1414 (2004).

Sitaxsentan CAS Registry Number: 184036-34-8 西他生坦

CAS Name: N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide
Additional Names: N-(4-chloro-3-methyl-5-isoxazolyl)-2-[3,4-(methylenedioxy)-6-meth...
Literature References: Selective endothelin A (ETA) receptor antagonist. Prepn: M. F. Chan et al., WO 9631492 ; eidem, US 5594021 (1996, 1997 both to Texas Biotech.); C. Wu et al., J. Med. Chem. 40, 1690 (1997). Pharmacology: R. G. Tilton et al., Pulm. Pharmacol. Ther. 13, 87 (2000). Clinical evaluation in heart failure: M. M. Givertz et al., Circulation 101, 2922 (2000); in pulmonary arterial hypertension: D. Langleben et al., Chest 126, 1377 (2004). Review of development and therapeutic potential: E. M. Horn et al., Expert Opin. Invest. Drugs 13, 1483-1492 (2004).

Gefitinib CAS Registry Number: 184475-35-2 吉非替尼

CAS Name: N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Additional Names: 4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazolineTrade...
Literature References: Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor which blocks signal transduction pathways implicated in the proliferation and survival of cancer cells. Prepn: K. H. Gibson, WO 9633980; idem, US 5770599 (1996, 1998 both to Zeneca). LC/MS/MS determn in biological samples: M. Zhao et al., J. Chromatogr. B 819, 73 (2005). Clinical pharmacokinetics and tolerability: H. Swaisland et al., Clin. Pharmacokinet. 40, 297 (2001). In vitro and in vivo inhibition of EGFR-expressing cancer lines: N. G. Anderson et al., Int. J. Cancer 94, 774 (2001). Proposed mechanism of action: A. Hirata et al., Cancer Res. 62, 2554 (2002). Clinical study in non-small cell lung cancer: M. G. Kris et al., J. Am. Med. Assoc. 290, 2149 (2003). Review: C. L. Arteaga, D. H. Johnson, Curr. Opin. Oncol. 13, 491-498 (2001). Review of clinical evaluations: D. Raben et al., Semin. Oncol. 29, Suppl. 4, 37-46 (2002); of use in non-small cell lung cancer: K. Tamura, M. Fukuoka, Expert Opin. Pharmacother. 6, 985-993 (2005).

Erlotinib CAS Registry Number: 183321-74-6 埃罗替尼

CAS Name: N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine
Percent Composition: C 67.16%, H 5.89%, N 10.68%, O 16.27%
Literature References: Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor. Prepn: R. C. Schnur, L. D. Arnold, WO 9630347; eidem, US 5747498 (1996, 1998 both to Pfizer). Mechanism of action study: J. D. Moyer et al., Cancer Res. 57, 4838 (1997). Enzyme inhibition and antitumor activity: V. A. Pollack et al., J. Pharmacol. Exp. Ther. 291, 739 (1999). HPLC determn in plasma: E. R. Lepper et al., J. Chromatogr. B 796, 181 (2003). Clinical pharmacokinetics: M. Hidalgo et al., J. Clin. Oncol. 19, 3267 (2001). Clinical evaluation in non-small-cell lung cancer: R. Pérez-Soler et al., J. Clin. Oncol. 22, 3238 (2004). Review of pharmacology and clinical development: T. E. Kim, J. R. Murren, Curr. Opin. Invest. Drugs 3, 1385-1395 (2002); and use in non-small cell lung cancer: F. H. Blackhall et al., Expert Opin. Pharmacother. 6, 995-1002 (2005).

Arzoxifene CAS Registry Number: 182133-25-1 阿佐昔芬

CAS Name: 2-(4-Methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]benzo[b]thiophene-6-ol
Additional Names: [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]2-(4-methoxyphenyl)]benzo[b]thiophe...
Literature References: Selective estrogen receptor modulator (SERM). Prepn: A. D. Palkowitz, K. J. Thrasher, EP 729956; idem, US 5981765 (1996, 1999 both to Eli Lilly). Pharmacology: M. Sato et al., Endocrinology 139, 4642 (1998); N. Suh et al., Cancer Res. 61, 8412 (2001). Clinical pharmacokinetics: P. N. Münster et al., J. Clin. Oncol. 19, 2002 (2001). Review of clinical evaluations and therapeutic potential: S. Chan, Semin. Oncol. 29, Suppl. 1, 129-133 (2002).

Gaboxadol CAS Registry Number: 64603-91-4 盐酸加波沙朵(THIP 盐酸盐)

CAS Name: 4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridin-3(2H)-one
Additional Names: 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol; THIPPercent Composition: C 51.42%, H 5.75%, N 19.99%, O 22.83%
Literature References: Selective extrasynaptic GABA agonist (SEGA); structural analog of muscimol, q.v. Prepn: P. Krogsgaard-Larsen, Acta Chem. Scand. B 31, 584 (1977); idem, EP 167; idem, US 4278676 (1979, 1981 both to H. Lundbeck Co.). GABA agonist effects: idem et al., Nature 268, 53 (1977). 3H-THIP binding study: E. Falch, P. Krogsgaard-Larsen, J. Neurochem. 38, 1123 (1982). HPLC determn: S. M. Madsen, J. Chromatogr. 238, 509 (1982). Pharmacokinetics: idem et al., Acta Pharmacol. Toxicol. 53, 353 (1983). Pharmacodynamics and potential therapeutic uses: A. V. Christensen et al., Pharm. Weekbl. Sci. Ed. 4, 145 (1982). Clinical effects on nocturnal sleep and hormone secretion: M. Lancel et al., Am. J. Physiol. Endocrinol. Metab. 281, E130 (2001); on night sleep and cognitive performance: S. Mathias et al., Neuropsychopharmacology 30, 833 (2005). Review of clinical development: R. Huckle, Curr. Opin. Invest. Drugs 5, 766-773 (2004).

Travoprost CAS Registry Number: 157283-68-6 曲伏前列腺素

CAS Name: (5Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[(1E,3R)-3-hydroxy-4-[3-(trifluoromethyl)phenoxy]-1-butenyl]cyclopentyl]-5-heptenoic acid 1-methylethyl ester
Additional Names: (+)-16-[3-(triflu...
Literature References: Selective FP prostaglandin receptor agonist. Isopropyl ester of (+)-fluprostenol, q.v. General prepn (not claimed): J. W. Stjernschantz, EP 364417 (1989 to Pharmacia). Large scale synthesis: L. T. Boulton et al., Org. Process Res. Dev. 6, 138 (2002). Pharmacology: M. R. Hellberg et al., J. Ocul. Pharmacol. Ther. 17, 421 (2001). LC/MS/MS determn in plasma: B. A. McCue et al., J. Pharm. Biomed. Anal. 28, 199 (2002). Ocular hypotensive effects in dogs: A. B. Carvalho et al., Vet. Ophthalmol. 9, 121 (2006). Clinical trial in glaucoma or ocular hypertension: R. L. Fellman et al., Ophthalmology 109, 998 (2002); in combination with timolol: J. S. Schuman et al., Am. J. Ophthalmol. 140, 242-250 (2005).