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

Enrofloxacin CAS Registry Number: 93106-60-6 恩诺沙星

CAS Name: 1-Cyclopropyl-7-(4-ethyl-1-piperazinyl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Additional Names: CFPQTrademarks: Baytril (Bayer)
Percent Composition: C 63.50%, H 6.1...
Literature References: Fluorinated quinolone antibacterial. Prepn: K. Grohe et al., DE 3142854; eidem, US 4670444 (1983, 1987 both to Bayer AG); K. Grohe, H. Heitzer, Ann. 1987, 29. Use as plant fungicide: K. Grohe et al., US 4563459 (1986 to Bayer AG). Pharmacokinetics in calves: J. N. Davidson et al., Proc. West. Pharmacol. Soc. 29, 129 (1986); in chickens: G. M. Conzelman et al., ibid. 30, 393 (1987). Spectrofluorometric determn of residues in poultry tissues: T. B. Waggoner, M. C. Bowman, J. Assoc. Off. Anal. Chem. 70, 813 (1987). Toxicology and physical properties: P. Altreuther, Vet. Med. Rev. 2, 87 (1987). Series of articles on pharmacology, in vitro antibacterial activity and field trials: ibid. 90-140.

Gatifloxacin CAS Registry Number: 112811-59-3 加替沙星

CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
Trademarks: Tequin (BMS); Zymar (Allergan)
Percent Composition: C 60.79%, H...
Literature References: Fluorinated quinolone antibacterial. Prepn: K. Masuzawa et al., EP 230295; eidem, US 4980470 (1987, 1990 both to Kyorin); J. P. Sanchez et al., J. Med. Chem. 38, 4478 (1995); of the sesquihydrate: T. Matsumoto et al., US 5880283 (1999 to Kyorin). In vitro antibacterial activity: A. Bauernfeind, J. Antimicrob. Chemother. 40, 639 (1997); H. Fukuda et al., Antimicrob. Agents Chemother. 42, 1917 (1998). Clinical pharmacokinetics: M. Nakashima et al., ibid. 39, 2635 (1995). Clinical study in urinary tract infection: H. Nito, 10th Mediterranean Congr. Chemother. 1996, 327; in respiratory tract infection: S. Sethi, Expert Opin. Pharmacother. 4, 1847 (2003).

Danofloxacin CAS Registry Number: 112398-08-0 达诺沙星

CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-3-quinolinecarboxylic acid
Percent Composition: C 63.85%, H 5.64%, F 5.32%, N 11.76%, O ...
Literature References: Fluorinated quinolone antibacterial. Prepn: M. R. Jefson, P. R. McGuirk, EP 215650; eidem, US 4861779 (1987, 1989 both to Pfizer). See also: F. R. Busch et al., EP 342849 (1989 to Pfizer), C.A. 113, 6177m (1990). Evaluation in treatment of pneumonia in cattle: W. T. R. Grimshaw et al., Dtsch. Tieraerztl. Wochenschr. 97, 529 (1990); C. J. Giles et al., Vet. Rec. 128, 296 (1991). Efficacy in treatment of E. coli diarrhoea in calves: S. J. Sunderland et al., Res. Vet. Sci. 74, 171 (2003).

Clinafloxacin CAS Registry Number: 105956-97-6 克林沙星

CAS Name: 7-(3-Amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Percent Composition: C 55.82%, H 4.68%, Cl 9.69%, F 5.19%, N 11.49%, O 13.12%
Literature References: Fluorinated quinolone antibacterial. Prepn: S. Suzue et al., EP 195316 (1986 to Kyorin). Antibacterial spectrum: M. S. Barrett et al., Diagn. Microbiol. Infect. Dis. 14, 389 (1991); S. M. H. Qadri et al., Chemotherapy (Basel) 38, 92 (1992).

Moxifloxacin CAS Registry Number: 151096-09-2 莫西沙星

CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid
Percent Composition: C 62.83%, H 6.03%, F 4.73%, N ...
Literature References: Fluorinated quinolone antibacterial. Prepn: U. Petersen et al., EP 550903 (1993 to Bayer). Antibacterial spectrum in vitro: J. M. Woodcock et al., Antimicrob. Agents Chemother. 41, 101 (1997). Activity vs Mycobacterium tuberculosis: B. Ji et al., ibid. 42, 2066 (1998). HPLC determn in serum: C. M. Tobin et al., J. Antimicrob. Chemother. 42, 278 (1998). Clinical pharmacokinetics: H. Stass et al., Antimicrob. Agents Chemother. 42, 2060 (1998). Review of pharmacology and clinical experience: M. Miravitlles, Expert Opin. Pharmacother. 6, 283-293 (2005).

Pefloxacin CAS Registry Number: 70458-92-3 培氟沙星

CAS Name: 1-Ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
Additional Names: pefloxacinePercent Composition: C 61.25%, H 6.05%, F 5.70%, N 12.61%, O 14.4...
Literature References: Fluorinated quinolone antibacterial; analog of norfloxacin, q.v. Prepn: M. Pesson, DE 2840910; idem, US 4292317 (1979, 1981 to Roger Bellon/Dainippon). Pharmacology and antibacterial spectrum: Y. Goueffon et al., C.R. Seances Acad. Sci. Ser. 3 292, 37 (1981). Pharmacokinetics: J. Barre et al., J. Pharm. Sci. 73, 1379 (1984). Bioavailability and metabolism: A. Contrepois et al., J. Antimicrob. Chemother. 14, 51 (1984); G. Montay et al., Antimicrob. Agents Chemother. 25, 463 (1984). HPLC determn in urine and plasma: eidem, J. Chromatogr. 272, 359 (1983). Adsorptive stripping voltammetry determn in bulk form, tablets and serum: A. M. Beltagi, J. Pharm. Biomed. Anal. 31, 1079 (2003). Symposium on pharmacokinetics, clinical efficacy and safety: J. Antimicrob. Chemother. 26, Suppl. B, 1-229 (1990).

Enoxacin CAS Registry Number: 74011-58-8 依诺沙星

CAS Name: 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acidTrademarks: Comprecin (Parke-Davis); Flumark (Dainippon)
Percent Composition: C 56.24%, H 5.35%...
Literature References: Fluorinated quinolone antibacterial; nalidixic acid analog. Prepn and antibacterial activity: J. Matsumoto et al., EP 9425; eidem, US 4352803; eidem, US 4359578 (1980, 1982, 1982 all to Dainippon and Roger Bellon); J. Matsumoto et al., J. Med. Chem. 27, 292 (1984). HPLC determn in plasma, urine: T. B. Vree et al., J. Chromatogr. 343, 449 (1985). In vitro comparison with other quinolones and azaquinolones: S. Selwyn, M. Bakhtiar, Drugs Exp. Clin. Res. 10, 653 (1984). Pharmacokinetics, therapeutic efficacy: K. G. Naber et al., Infection 13, 219 (1985). Efficacy in treatment of urinary tract infections: R. R. Bailey, B. A. Peddie, N. Z. Med. J. 98, 286 (1985). Toxicology studies: H. Senda et al., Chemotherapy (Tokyo) 32, Suppl. 3, 192 (1984). Series of articles on activity, pharmacology, metabolism, early clinical studies: ibid. 1-1093; J. Antimicrob. Chemother. 14, Suppl. C, 1-96 (1984); on activity, pharmacokinetics, clinical safety and efficacy: Infection 14, Suppl. 3, S183-S220 (1986).

Pazufloxacin CAS Registry Number: 127045-41-4 帕珠沙星

CAS Name: (3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acidPercent Composition: C 60.37%, H 4.75%, F 5.97%, N 8.80%, O 20.11%
Literature References: Fluorinated quinolone. Prepn: H. Narita et al., DE 3913245; eidem, US 4990508 (1989, 1991 both to Toyama). Synthesis: Y. Todo et al., Chem. Pharm. Bull. 42, 2569 (1994). Antimicrobial activity: Y. Fukuoka et al., Antimicrob. Agents Chemother. 37, 384 (1993).

Rufloxacin CAS Registry Number: 101363-10-4 如氟沙星

CAS Name: 9-Fluoro-2,3-dihydro-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzothiazine-6-carboxylic acidPercent Composition: C 56.18%, H 4.99%, F 5.23%, N 11.56%, O 13.21%, S 8.82%
Literature References: Fluorinated quinolone; structurally similar to ofloxacin, q.v. Prepn: G. Mascellani et al., AU 85 39142; eidem, US 4684647 (1985, 1987 both to Mediolanum); V. Cecchetti et al., J. Med. Chem. 30, 465 (1987). In vitro activity: R. Wise et al., Antimicrob. Agents Chemother. 29, 649 (1992). Mechanism of action and resistance: L. J. V. Piddock et al., J. Antimicrob. Chemother. 31, 855 (1993). Pharmacokinetics and safety: J. C. Kisicki et al., ibid. 36, 1296 (1992). HPLC determn in biological fluids: F. Lombardi et al., J. Chromatogr. 576, 129 (1992). Clinical study in cystitis and urinary tract infections: R. Mattina et al., Infection 21, 106 (1993); in bronchitis: W. Klietmann et al., Antimicrob. Agents Chemother. 37, 2298 (1993).

Flubendazole CAS Registry Number: 31430-15-6 氟苯咪唑

CAS Name: [5-(4-Fluorobenzoyl)-1H-benzimidazol-2-yl]carbamic acid methyl ester
Additional Names: 5-(p-fluorobenzoyl)-2-benzimidazolecarbamic acid methyl esterTrademarks: Flubenol (J J); Flumox...
Literature References: Fluoro analog of mebendazole, q.v. Prepn: J. L. H. Van Gelder et al., DE 2029637; eidem, US 3657267 (1971, 1972 both to Janssen); A. H. M. Raeymaekers et al., Arzneim.-Forsch. 28, 586 (1978). Pharmacological, biological properties: D. Thienpont et al., ibid. 605. Anthelmintic activity in rats: O. Vanparijs et al., Vet. Parasitol. 5, 237 (1979); in pigs: E. Telléz-Giron et al., Am. J. Trop. Med. Hyg. 30, 135 (1981).