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

Indomethacin CAS Registry Number: 53-86-1 吲哚美辛

CAS Name: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid
Additional Names: 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid; indometacin
Trademarks: Bonidon (Mepha...
Literature References: Nonsteroidal anti-inflammatory agent (NSAID); inhibits prostaglandin synthesis. Prepn: T. Y. Shen et al., J. Am. Chem. Soc. 85, 488 (1963); T. Y. Shen, US 3161654 (1964 to Merck Co.). Alternate process: BE 679678 (1966 to Sumitomo). Anti-inflammatory and antipyretic activity: C. A. Winter et al., J. Pharmacol. Exp. Ther. 141, 369 (1963). Metabolic studies: D. W. Yesair et al., Biochem. Pharmacol. 19, 1579 (1970). Toxicity: C. D. Klaassen, Toxicol. Appl. Pharmacol. 38, 127 (1976). Review of discovery, pharmacology and mechanism of action: T. Y. Shen, C. A. Winter in Advances in Drug Research vol. 12, A. B. Simmons, Ed. (Academic Press, New York, 1977) pp 89-245; of clinical trials in osteoarthritis: W. M. O'Brien, Clin. Pharmacol. Ther. 9, 94-107 (1968); of role in ductus closure: S. M. Douidar et al., Dev. Pharmacol. Ther. 11, 196-212 (1988).

Indoprofen CAS Registry Number: 31842-01-0 吲哚布洛芬

CAS Name: 4-(1,3-Dihydro-1-oxo-2H-isoindol-2-yl)-a-methylbenzeneacetic acid
Additional Names: p-(1-oxo-2-isoindolinyl)hydratropic acid; 2-[4-(1-carboxyethyl)phenyl]-1-isoindolinone; 1-oxo-2-[p-...
Literature References: Nonsteroidal anti-inflammatory agent. Prepn: BE 753600; R. W. J. Carney, G. de Stevens, US 4316850 (1970, 1982 both to Ciba); P. N. Giraldi et al., DE 2154525 (1972 to Carlo Erba), C.A. 77, 88292v (1972); G. Nannini et al., Arzneim.-Forsch. 23, 1090 (1973). Synthesis and resolution of enantiomers: F. Buzzetti et al., DE 2258088 (1974 to Carlo Erba), C.A. 81, 13382y (1974); T. Kametani et al., J. Heterocycl. Chem. 15, 369 (1978). Abs config: S. De Munari et al., Tetrahedron Lett. 21, 2273 (1980). Pharmacology: A. Buttinoni et al., Arzneim.-Forsch. 23, 1100 (1973). Absorption, excretion and metabolism: G. C. Goldaniga et al., ibid. 24, 1603 (1974); L. F. Chasseaud et al., ibid. 1606. GLC determn of enantiomers in plasma: G. P. Tosolini et al., J. Pharm. Sci. 63, 1072 (1974). Biological activity and toxicity data: A. Buttinoni et al., J. Pharm. Pharmacol. 35, 603 (1983).

Tenoxicam CAS Registry Number: 59804-37-4 替诺昔康

CAS Name: 4-Hydroxy-2-methyl-N-2-pyridinyl-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamide 1,1-dioxideTrademarks: Alganex (Roche); Dolmen (Sigma-Tau); Liman (Kali-Chemie); Mobiflex (Roche); Rexalgan (...
Literature References: Nonsteroidal anti-inflammatory agent. Prepn: O. Hromatka et al., DE 2537070 (1976 to Hoffmann-La Roche), C.A. 85, 63077 (1976). Pharmacology: Y. Tanaka et al., Nippon Yakurigaku Zasshi 77, 531 (1981), C.A. 95, 35473 (1981). HPLC determn in plasma: M. E. Pickup et al., J. Chromatogr. 225, 493 (1981). Comparative study vs aspirin in normal volunteers: H. A. Bird et al., Curr. Med. Res. Opin. 8, 9 (1982). Preliminary review of pharmacology, therapeutic efficacy and mechanism of action: J. P. Gonzalez, P. A. Todd, Drugs 34, 289-310 (1987). Comprehensive description: A. M. Al-Obaid, M. S. Mian, Anal. Profiles Drug Subs. Excip. 22, 431-459 (1993).

Isofezolac CAS Registry Number: 50270-33-2 三苯唑酸

CAS Name: 1,3,4-Triphenyl-1H-pyrazole-5-acetic acidTrademarks: Sofenac (Rhe-Poulenc)
Percent Composition: C 77.95%, H 5.12%, N 7.90%, O 9.03%
Literature References: Non-steroidal anti-inflammatory agent; prostaglandin synthetase inhibitor. Prepn: C. Gueremy, C. Renault, DE 2312256; eidem, US 3984431 (1973, 1976 to Société Générale de Recherches et d'Applications Scientifiques). Pharmacology: J. Mizoule et al., Arch. Int. Pharmacodyn. 238, 305 (1979). HPLC determn in biological fluids: A. Bannier et al., J. Chromatogr. 227, 213 (1982).

Isoxicam CAS Registry Number: 34552-84-6 伊索昔康

CAS Name: 4-Hydroxy-2-methyl-N-(5-methyl-3-isoxazolyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
Additional Names: 4-hydroxy-3-(5-methyl-3-isoxazolocarbamyl)-2-methyl-2H-1,2-benzothiazine ...
Literature References: Nonsteroidal anti-inflammatory drug with antipyretic and analgesic properties. Prepn: H. Zinnes et al., DE 2208351; eidem, US 3787324 (1972, 1974 both to Warner-Lambert). Anti-inflammatory properties: G. DiPasquale et al., Agents Actions 5, 256 (1975); ibid. 6, 748 (1976). Pharmacological studies: G. DiPasquale, D. Mellace, ibid. 7, 481 (1977); K. Rainsford, ibid. 573; G. DiPasquale et al., Res. Commun. Chem. Pathol. Pharmacol. 19, 529 (1978). Pharmacokinetics in man: E. U. Kölle et al., Arzneim.-Forsch. 33, 582 (1983). Review of safety and toxicity: M. W. Whitehouse, Br. J. Clin. Pharmacol. 22, 111S-116S (1986). Series of articles on pharmacology, safety and clinical efficacy: Am. J. Med. 79, Suppl. 4B, 1-42 (1985); Br. J. Clin. Pharmacol. 22, Suppl. 2, 107S-190S (1986). Review: Semin. Arthritis Rheum. 12, Suppl. 2, 153-183 (1982).

Feprazone CAS Registry Number: 30748-29-9 非普拉宗

CAS Name: 4-(3-Methyl-2-butenyl)-1,2-diphenyl-3,5-pyrazolidinedione
Additional Names: 4-prenyl-1,2-diphenyl-3,5-pyrazolidinedione; 4-prenyl-1,2-diphenyl-3,5-dioxopyrazolidine; 4-(b-isoamylenyl)...
Literature References: Non-steroidal anti-inflammatory drug. Prepn: S. Casadio, G. Pala, DE 2031238; eidem, US 3703528 (1971, 1972 both to Ist. De Angeli); Casadio et al., Arzneim.-Forsch. 22, 171 (1972). Series of articles on physical-chemical data, pharmacology, toxicology and clinical studies: ibid. 174-281. Toxicity data: C. Bianchi, G. Bonardi, ibid. 196.

Loxoprofen CAS Registry Number: 68767-14-6 洛索洛芬

CAS Name: a-Methyl-4-[(2-oxocyclopentyl)methyl]benzeneacetic acid
Additional Names: (±)-p-[(2-oxocyclopentyl)methyl]hydratropic acid
Percent Composition: C 73.15%, H 7.37%, O 19.49%
Literature References: Non-steroidal anti-inflammatory pro-drug; the active metabolite is the trans-cyclohydroxypentane. Prepn of racemate: A. Terada et al., DE 2814556; eidem, US 4161538 (1978, 1979 both to Sankyo); of enantiomers: A. Terada, E. Misaka, EP 55588; eidem, US 4400534 (1982, 1983 both to Sankyo). Use as topical anti-inflammatory: A. Terada et al., BE 889149 (1981 to Sankyo), C.A. 96, 199326w (1982). Metabolism: Y. Tanaka et al., Chem. Pharm. Bull. 31, 3656 (1983); eidem, ibid. 32, 1040 (1984). Structure of metabolites: S. Naruto et al., ibid. 258. Optical inversion of (2R)- to (2S)-isomer after oral administration to rats: H. Nagashima et al., ibid. 251. Inhibition of in vivo and in vitro prostaglandin synthesis: K. Matsuda et al., Biochem. Pharmacol. 33, 2473 (1984).

Nepafenac CAS Registry Number: 78281-72-8 奈帕芬胺

CAS Name: 2-Amino-3-benzoylbenzeneacetamideTrademarks: Nevanac (Alcon)
Percent Composition: C 70.85%, H 5.55%, N 11.02%, O 12.58%
Literature References: Nonsteroidal anti-inflammatory with analgesic activity; selective COX-2 inhibitor. Prodrug of amfenac, q.v. Prepn: D. A. Walsh et al., DE 3035688 (1981 to A. H. Robins); see also: J. R. Shanklin, Jr. et al., US 4313949 (1982 to A. H. Robins); D. A. Walsh et al., J. Med. Chem. 33, 2296 (1990). Ocular pharmacology: D. A. Gamache et al., Inflammation 24, 357 (2000); T.-L. Ke et al., ibid. 371. Inhibition of ocular neovascularization: K. Takahashi et al., Invest. Ophthalmol. Visual Sci. 44, 409 (2003). Review of clinical experience: R. Lindstrom, T. Kim, Curr. Med. Res. Opin. 22, 397-404 (2006).

Isoxepac CAS Registry Number: 55453-87-7 伊索克酸

CAS Name: 6,11-Dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid
Additional Names: oxepinacTrademarks: Artil (Hoechst)
Percent Composition: C 71.64%, H 4.51%, O 23.86%
Literature References: Non-steroidal anti-inflammatory with analgesic and antipyretic activity. Prepn: K. Ueno et al., JP Kokai 74 124086 (1974 to Daiichi), C.A. 82, 170735d (1975); G. C. Helsley et al., DE 2442060; eidem, US 4585788 (1975, 1986 both to Hoechst); K. Ueno et al., J. Med. Chem. 19, 941 (1976); D. E. Aultz et al., ibid. 20, 66 (1977). Pharmacology: H. B. Lassman et al., Arch. Int. Pharmacodyn. Ther. 227, 142 (1977). Disposition and metabolism in animals and humans: H. P. A. Illing, J. M. Fromson, Drug Metab. Dispos. 6, 510 (1978). HPLC determn in plasma: J. A. Slack, J. Chromatogr. 221, 431 (1980); H. K. L. Hundt, L. W. Brown, ibid. 225, 482 (1981). Clinical studies: S. Sasaki, Arzneim.-Forsch. 28, 462 (1978); L. B. Svendsen et al., Scand. J. Rheumatol. 10, 186 (1981); J. Scott, E. C. Huskisson, Rheumatol. Rehabil. 21, 48 (1982).

Piroxicam CAS Registry Number: 36322-90-4 吡罗昔康

CAS Name: 4-Hydroxy-2-methyl-N-2-pyridinyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
Additional Names: 3,4-dihydro-2-methyl-4-oxo-N-2-pyridyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide...
Literature References: Non-steroidal anti-inflammatory with long half-life. Prepn (keto form): J. Lombardino, DE 1943265; idem, US 3591584 (1970, 1971 to Pfizer). Synthesis and biological properties: J. Lombardino, E. Wiseman, J. Med. Chem. 15, 848 (1972); J. Lombardino et al., ibid. 16, 493 (1973). Pharmacology: E. Wiseman et al., Arzneim.-Forsch. 26, 1300 (1976). Evaluation of ulcerogenic effects: G. Palacios et al., Methods Find. Exp. Clin. Pharmacol. 9, 353 (1987). Clinical pharmacology: L. Martinez et al., ibid. 10, 729 (1988). Review: eidem, in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 324-346. Review of pharmacology and therapeutic efficacy: R. N. Brogden et al., Drugs 22, 165-187 (1981); eidem, ibid. 28, 292-323 (1984). Symposium on clinical efficacy and safety: Am. J. Med. 81, Suppl. 5B, 1-55 (1986). Comprehensive description: M. Mihalic et al., Anal. Profiles Drug Subs. 15, 509-531 (1986).