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

Warburganal CAS Registry Number: 62994-47-2 1,2-萘二羧醛,1,4,4a,5,6,7,8a-辛氢-1-羟基-5,5,8a-三甲基-, (1S,4aS,8aS)-

CAS Name: (1S,4aS,8aS)-1,4,4a,5,6,7,8,8a-Octahydro-1-hydroxy-5,5,8a-trimethyl-1,2-naphthalenedicarboxaldehyde
Percent Composition: C 71.97%, H 8.86%, O 19.17%
Literature References: Drimane sesquiterpene with antifeedant activity against the African army worm. Biological activity includes plant growth regulation, cytotoxic, antimicrobial and molluscicidal properties. Isoln from Warburgia ugandensis, Canellaceae and structure: I. Kubo et al., Chem. Commun. 1976, 1013. Relationship between structure and antifeedant activity: K. Nakanishi, I. Kubo, Isr. J. Chem. 16, 28 (1977). Synthesis of (±)-warburganal: S. P. Tanis, K. Nakanishi, J. Am. Chem. Soc. 101, 4398 (1979); T. Nakata et al., ibid. 4400; A. S. Kende, T. J. Blacklock, Tetrahedron Lett. 1980, 3119; P. A. Wender, S. L. Eck, ibid. 1982, 1871; D. M. Hollinshead et al., J. Chem. Soc. Perkin Trans. 1 1983, 1579. See also: JP Kokai 80 136238, and JP 80 136240 (both 1980 to Inst. Phys. Chem. Res.); JP Kokai 81 43236 (1981 to Suntory Ltd.); JP Kokai 83 38232 (1983 to Teikoku Zoki). Synthesis of (-)-warburganal: H. Okawara et al., Tetrahedron Lett. 1982, 1087.

Caro's Acid CAS Registry Number: 7722-86-3 过氧单硫酸

CAS Name: Peroxymonosulfuric acid
Additional Names: sulfomonoperacid; persulfuric acid
Percent Composition: H 1.77%, O 70.12%, S 28.11%
Literature References: Dry reagent is prepd by stirring 10 g potassium persulfate into 11 g concd H2SO4 for 10 min and adding 30 g finely powdered potassium sulfate; liquid reagent is obtained by triturating potassium persulfate with three times as much (by weight) of H2SO4; dil reagent is prepd by stirring 10 g potassium persulfate into 11 g concd H2SO4 and adding 50 cc ice: Baeyer, Villiger, Ber. 32, 3625 (1899); another prepn by reacting 90% H2O2 with chlorosulfonic acid at -40 to -50°: Ball, Edwards, J. Am. Chem. Soc. 78, 1125 (1956).

Olopatadine CAS Registry Number: 113806-05-6 奥洛他定

CAS Name: (11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid
Percent Composition: C 74.75%, H 6.87%, N 4.15%, O 14.23%
Literature References: Dual acting histamine H1-receptor antagonist and mast cell stabilizer. Prepn: E. Oshima et al., EP 235796; eidem, US 5116863 (1987, 1992 both to Kyowa); eidem, J. Med. Chem. 35, 2074 (1992). Pharmacology: C. Kamei et al., Arzneim.-Forsch. 45, 1005 (1995); J. M. Yanni et al., J. Ocul. Pharmacol. Ther. 12, 389 (1996). Receptor binding profile: N. A. Sharif et al., J. Pharmacol. Exp. Ther. 278, 1252 (1996). Clinical trial in allergic conjunctivitis: M. B. Abelson, L. Spitalny, Am. J. Ophthalmol. 125, 797 (1998).

Rupatadine CAS Registry Number: 158876-82-5 芦帕他定

CAS Name: 8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridinePercent Composition: C 75.07%, H 6.30%, Cl 8.52%, N 10.10%
Literature References: Dual antagonist of histamine H1 and platelet-activating factor receptors. Prepn: E. Carceller et al., ES 2042421; eidem, US 5407941 (1993, 1995 both to Uriach); eidem, J. Med. Chem. 37, 2697 (1994). Mechanism of action: M. Merlos et al., J. Pharmacol. Exp. Ther. 280, 114 (1997). Clinical trial in seasonal allergic rhinitis: F. Saint-Martin et al., J. Invest. Allergol. Clin. Immunol. 14, 34 (2004); and comparison with ebastine: E. M. Guadaño et al., Allergy 59, 766 (2004). Review of pharmacology and clinical development: N. Y. Van Den Anker-Rakhmanina, Curr. Opin. Anti-Inflam. Immunomod. Invest. Drugs 2, 127-132 (2000).

Tezosentan CAS Registry Number: 180384-57-0 替唑生坦

CAS Name: N-[6-(2-Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(1H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-(1-methylethyl)-2-pyridinesulfonamide
Additional Names: 5-isopropylpyridine-2-sulfoni...
Literature References: Dual endothelin (ETA/ETB) receptor antagonist. Prepn: V. Breu et al., WO 9619459; eidem, US 6004965 (1996, 1999 both to Hoffmann-La Roche). Pharmacology and receptor binding: M. Clozel et al., J. Pharmacol. Exp. Ther. 290, 840 (1999). Clinical pharmacokinetics: J. Dingemanse et al., Br. J. Clin. Pharmacol. 53, 355 (2002). Clinical evaluation in advanced heart failure: C. Schalcher et al., Am. Heart J. 142, 340 (2001). LC-MS determn in plasma: P. L. M. van Giersbergen et al., J. Chromatogr. B 792, 369 (2003).

Dutasteride CAS Registry Number: 164656-23-9 度他雄胺

CAS Name: (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-[2,5-Bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-1H-indeno[5,4-f]quinoline-7-carboxamide
Addit...
Literature References: Dual inhibitor of 5a-reductase isoenzymes types 1 and 2; structurally related to finasteride, q.v. Prepn: K. W. Batchelor, S. V. Frye, WO 9507927 (1995 to Glaxo). Structure-activity study: R. K. Bakshi et al., J. Med. Chem. 38, 3189 (1995). Clinical pharmacokinetics: P. O. Gisleskog et al., Br. J. Clin. Pharmacol. 47, 53 (1999). Clinical trial in benign prostatic hyperplasia: C. G. Roehrborn et al., Urology 60, 434 (2002). Review of discovery and development: S. V. Frye et al., Pharm. Biotechnol. 11, 393-422 (1998); of clinical experience: B. Djavan et al., Expert Opin. Pharmacother. 6, 311-317 (2005).

Licofelone CAS Registry Number: 156897-06-2 利克飞龙

CAS Name: 6-(4-Chlorophenyl)-2,3-dihydro-2,2-dimethyl-7-phenyl-1H-pyrrolizine-5-acetic acidPercent Composition: C 72.72%, H 5.84%, Cl 9.33%, N 3.69%, O 8.42%
Literature References: Dual inhibitor of cyclooxygenase and 5-lipoxygenase. Prepn: G. Dannhardt et al., EP 397175; eidem, US 5260451 (1990, 1993 both to Merckle); S. A. Laufer et al., J. Med. Chem. 37, 1894 (1994); J. Cossy, D. Belotti, Tetrahedron 55, 5145 (1999). Mechanism of action: S. Tries et al., Inflamm. Res. 51, 135 (2002). Experience in experimental dog osteoarthritis: D. Lajeunesse et al., Ann. Rheum. Dis. 63, 78 (2004). Gastrointestinal safety profile in dogs: M. Moreau et al., J. Vet. Pharmacol. Ther. 28, 81 (2005). Review of clinical development: S. Laufer, Inflammopharmacology 9, 101-112 (2001); J. M. Alvaro-Gracia, Rheumatology 43, Suppl. 1, i21-i25 (2004).

Tepoxalin CAS Registry Number: 103475-41-8 替泊沙林

CAS Name: 5-(4-Chlorophenyl)-N-hydroxy-1-(4-methoxyphenyl)-N-methyl-1H-pyrazole-3-propanamide
Additional Names: 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-methylpropanam...
Literature References: Dual inhibitor of cyclooxygenase and 5-lipoxygenase. Prepn: M. P. Wachter, M. P. Ferro, EP 248594; eidem, US 4826868 (1987, 1989, both to Ortho); W. V. Murray, S. K. Hadden, J. Org. Chem. 57, 6662 (1992). LC/MS characterization of impurities and degradation products: D. J. Burinsky et al., J. Pharm. Sci. 85, 159 (1996). Mechanism of action: S. S. C. Tam et al., J. Biol. Chem. 270, 13948 (1995). Toxicity study in rats, dogs: E. V. Knight et al., Fundam. Appl. Toxicol. 33, 38 (1996). Pharmacological profile in animal models: D. C. Argentieri et al., J. Pharmacol. Exp. Ther. 271, 1399 (1994); in man: M. Depré et al., Int. J. Clin. Pharmacol. Res. 16, 1 (1996). Bioavailability in dogs: L. M. Homer et al., J. Vet. Pharmacol. Ther. 28, 287 (2005).

Omapatrilat CAS Registry Number: 167305-00-2 奥马曲拉

CAS Name: (4S,7S,10aS)-Octahydro-4-[[(2S)-2-mercapto-1-oxo-3-phenylpropyl]amino]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acidTrademarks: Vanlev (BMS)
Percent Composition: C 55.86%, H...
Literature References: Dual metalloprotease inhibitor of neutral endopeptidase (NEP) and angiotensin converting enzyme (ACE). Prepn: J. A. Robl et al., EP 629627; idem, US 5508272 (1994, 1996 both to Bristol-Myers Squibb); and pharmacological evaluation: idem et al., J. Med. Chem. 40, 1570 (1997). HPLC-MS determn in rat plasma: M. Jemal, D. J. Hawthorne, J. Chromatogr. B 698, 123 (1997). Antihypertensive activity in rats: N. C. Trippodo et al., Am. J. Hypertens. 11, 363 (1998). Clinical pharmacodynamics: C. Massien et al., Clin. Pharmacol. Ther. 65, 448 (1999). Review of pharmacology and clinical use: M. Weber, Am. J. Hypertens. 12, 139S-147S (1999). Clinical trial in heart failure: J. L. Rouleau et al., Lancet 356, 615 (2000).

Sarizotan CAS Registry Number: 351862-32-3 N-((3,4-二氢-2H-1-苯并吡喃-2-基)甲基)-5-(4-氟苯基)-3-吡啶甲基胺

CAS Name: N-[[(2R)-3,4-Dihydro-2H-1-benzopyran-2-yl]methyl]-5-(4-fluorophenyl)-3-pyridinemethanamine
Additional Names: (R)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chromane; (R)-(-)...
Literature References: Dual serotonin 5-HT1A receptor agonist and dopamine D2 receptor antagonist. Prepn: H. Böttcher et al., EP 707007; eidem, US 5767132 (1996, 1998 both to Merck Patent GmbH). PET receptor binding study: E. A. Rabiner et al., J. Psychopharmacol. 16, 195 (2002). Neurochemical profile: G. D. Bartoszyk et al., J. Neural Transm. 111, 113 (2004). Clinical evaluation in dyskinesia in Parkinson's disease: C. W. Olanow et al., Clin. Neuropharmacol. 27, 58 (2004); W. Bara-Jimenez et al., Mov. Disord. 20, 932 (2005).