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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

  • Doxifluridine CAS Registry Number: 3094-09-5 去氧氟尿苷


    CAS Name: 5'-Deoxy-5-fluorouridine
    Additional Names: 1-(b-D-5'-deoxyribofuranosyl)-5-fluorouracil; 5'-DFUR; 5'-dFUrdTrademarks: Flutron (Roche); Furtulon (Roche)
    Percent Composition: C 43.91...
    Literature References: Fluorinated pyrimidine nucleoside with cytostatic activity. Prepn: A. F. Cook, US 4071680 (1978 to Hoffmann-La Roche); H. Hrebabecky, J. Beranek, Nucleic Acids Res. 5, 1029 (1978); A. F. Cook et al., J. Med. Chem. 22, 1330 (1979). Stereospecific synthesis: J. Kiss et al., Helv. Chim. Acta 65, 1522 (1982). Mechanism of action studies: H.-R. Hartmann, A. Matter, Cancer Res. 42, 2412 (1982); R. D. Armstrong et al., Cancer Chemother. Pharmacol. 11, 102 (1983). Kinetics and metabolism in humans: J.-P. Sommadossi et al., Cancer Res. 43, 930 (1983). Clinical trials in colorectal carcinoma: R. Abele et al., J. Clin. Oncol. 1, 750 (1983); S. D. Fossa et al., Cancer Chemother. Pharmacol. 15, 161 (1985). Series of articles on animal toxicology: Yakuri to Chiryo 13, Suppl. 2, 221-430 (1985); acute toxicity: M. Shimizu et al., ibid. 209, C.A. 104, 14673z-14678e (1986). Evaluation of neurotoxicity in humans: M. S. Heier, S. D. Fossa, Acta Neurol. Scand. 73, 449 (1986).

  • Orbifloxacin CAS Registry Number: 113617-63-3 奥比沙星


    CAS Name: rel-1-Cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-5,6,8-trifluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
    Additional Names: 1-cyclopropyl-5,6,8-trifluoro-(cis-3,5-dimethy...
    Literature References: Fluorinated quinoline antibacterial. Prepn: J. Matsumoto et al., EP 242789; eidem, US 4886810 (1987, 1989 both to Dainippon). In vitro activity vs Staphylococcus intermedius: J.-P. Ganière et al., Res. Vet. Sci. 77, 67 (2004). Photodegradation kinetics: T. Morimura et al., Chem. Pharm. Bull. 43, 1000 (1995). Pharmacokinetics in mares: G. R. Haines et al., Can. J. Vet. Res. 65, 181 (2001). HPLC determn in rabbit plasma: M. A. Garcia et al., J. Chromatogr. Sci. 37, 199 (1999); LC/fluorescence/MS determn in eggs: M. J. Schneider, D. J. Donoghue, Anal. Chim. Acta 483, 39 (2003). Localization of drug to diseased skin: P. A. Kay-Mugford et al., Vet. Ther. 3, 1 (2002). Review of veterinary use in Japan: S. Nakamura, Drugs 49, Suppl. 2, 152-158 (1995); of use in companion animals: R. D. Walker, Aust. Vet. J. 78, 84-90 (2000).

  • Lomefloxacin CAS Registry Number: 98079-51-7 洛美沙星


    CAS Name: 1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
    Percent Composition: C 58.11%, H 5.45%, F 10.81%, N 11.96%, O 13.66%
    Literature References: Fluorinated quinolone antibacterial. DNA gyrase antagonist. Prepn: Y. Itoh et al., DE 3433924; eidem, US 4528287 (both 1985 to Hokuriku Pharm.). In vitro and in vivo activity: T. Hirose et al., Antimicrob. Agents Chemother. 31, 854 (1987). Comparative antibacterial spectrum in vitro: R. Wise et al., ibid. 32, 617 (1988). HPLC determn in urine and bile and preliminary pharmacokinetics in rats: A. Saito et al., ibid. 156. Photochemistry study: E. Fasani et al., Eur. J. Org. Chem.2004, 5075. Supplement on antibacterial spectrum, pharmacokinetics and clinical efficacy: Chemotherapy (Tokyo) 36, Suppl. 2, 1-1418 (1988). Comprehensive description: Y. D. Sanzgiri et al., Anal. Profiles Drug Subs. Excip. 23, 321-369 (1994).

  • Fleroxacin CAS Registry Number: 79660-72-3 氟罗沙星


    CAS Name: 6,8-Difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acidTrademarks: Megalocin (Roche); Megalone (Roche); Quinodis (Roche)
    Percent Composi...
    Literature References: Fluorinated quinolone antibacterial. Prepn: BE 887574; T. Irikura et al., US 4398029 (1981, 1983 both to Kyorin). Antibacterial spectrum in vitro and in vivo: K. Hirai et al., Antimicrob. Agents Chemother. 29, 1059 (1986). In vitro activity vs anaerobic bacteria: J. Wüst, U. Hardegger, Eur. J. Clin. Microbiol. 6, 688 (1987). HPLC determn in biological fluids: H. Kusajima et al., J. Chromatogr. 381, 137 (1986). Pharmacokinetics and bioavailability: E. Weidekamm et al., Antimicrob. Agents Chemother. 31, 1909 (1987). Preliminary clinical evaluation in gonorrhea: J. B. J. Boerema et al., J. Antimicrob. Chemother. 21, 140 (1988).

  • Sarafloxacin CAS Registry Number: 98105-99-8 沙拉沙星


    CAS Name: 6-Fluoro-1-(4-fluorophenyl)-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid
    Percent Composition: C 62.33%, H 4.45%, F 9.86%, N 10.90%, O 12.46%
    Literature References: Fluorinated quinolone antibacterial. Prepn: D. T. W. Chu, EP 131839; idem, US 4730000 (1985, 1988 both to Abbott); D. T. W. Chu et al., J. Med. Chem. 28, 1558 (1985); H. Narita et al., JP Kokai 85 237069 (1985 to Toyama). Comparative in vitro antibacterial spectrum: A. Digranes, W. L. Dibb, Chemotherapy 34, 298 (1988). In vivo antibacterial activity: P. B. Fernandes et al., Antimicrob. Agents Chemother. 29, 201 (1986). HPLC determn: J. F. Bauer et al., Pharm. Res. 7, 1177 (1990).

  • Nadifloxacin CAS Registry Number: 124858-35-1 那氟沙星


    CAS Name: 9-Fluoro-6,7-dihydro-8-(4-hydroxy-1-piperidinyl)-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acid
    Additional Names: jinofloxacinTrademarks: Acuatim (Otsuka)
    Percent Comp...
    Literature References: Fluorinated quinolone antibacterial. Prepn: H. Ishikawa et al., BE 891046; eidem, US 4399134 (1982, 1983 both to Otsuka); eidem, Chem. Pharm. Bull. 37, 2103 (1989). Toxicity data: K. Hashimoto et al., Iyakuhin Kenkyu 21, 671 (1990), C.A. 114, 156625r (1991). In vitro antibacterial activity: K. Vogt et al., Eur. J. Clin. Microbiol. Infect. Dis. 11, 943 (1992). HPLC determn: M. Koike et al., J. Chromatogr. 526, 235 (1990). Clinical trial in treatment of acne: I. Kurokawa et al., J. Am. Acad. Dermatol. 25, 674 (1991).

  • Balofloxacin CAS Registry Number: 127294-70-6 巴洛沙星


    CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidinyl]-4-oxo-3-quinolinecarboxylic acidTrademarks: Baloxin (Chugai)
    Percent Composition: C 61.69%, H 6.21%, F 4...
    Literature References: Fluorinated quinolone antibacterial. Prepn: H. Nagano et al., EP 342675; eidem, US 5051509 (1989, 1991 both to Chugai). Photostability: K. Marutani et al., Antimicrob. Agents Chemother. 37, 2217 (1993). Comparative antibacterial spectrum: H. Iwasaki et al., Chemotherapy (Basel) 41, 100 (1995). Pharmacokinetics: T. Nakagawa et al., Arzneim.-Forsch. 45, 719 (1995). HPLC determn in biological fluids: T. Nakagawa et al., ibid. 716. Clinical evaluation in respiratory tract infection: O. Kunii, F. Matsumoto, Proc. 18th Int. Congr. Chemother., Stockholm 1993, 22-23; in urinary tract infection: J. Kumazawa, F. Matsumoto, ibid., 69-70.

  • Grepafloxacin CAS Registry Number: 119914-60-2 格帕沙星


    CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
    Percent Composition: C 63.50%, H 6.17%, F 5.29%, N 11.69%, O 13.36%
    Literature References: Fluorinated quinolone antibacterial. Prepn: J. M. Domagala et al., WO 8906649; eidem, US 4920120 (1989, 1990 both to Warner-Lambert); S. E. Hagen et al., J. Med. Chem. 34, 1155 (1991). Comparative in vitro activity: F. Marco et al., J. Antimicrob. Chemother. 33, 647 (1994); R. C. Arduino et al., ibid. 34, 403. HPLC determn in human bronchoalveolar lavage samples: J. M. Woodcock et al., FEMS Microbiol. Lett. 119, 315 (1994). Clinical pharmacokinetics: J. Child et al., Antimicrob. Agents Chemother. 39, 513 (1995). Tissue concentration in lung: P. J. Cook et al., J. Antimicrob. Chemother. 35, 317 (1995). Review of pharmacology and clinical trials: A. J. Wagstaff, J. A. Balfour, Drugs 53, 817-824 (1997).

  • Sparfloxacin CAS Registry Number: 110871-86-8 司帕沙星


    CAS Name: rel-5-Amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acidTrademarks: Spara (Dainippon); Zagam (Specia)
    Percent Composi...
    Literature References: Fluorinated quinolone antibacterial. Prepn: J. Matsumoto et al., EP 221463; eidem, US 4795751 (1987, 1989 both to Dainippon). Synthesis and structure-activity relationship: T. Miyamoto et al., J. Med. Chem. 33, 1645 (1990). Antibacterial activity: S. Nakamura et al., Antimicrob. Agents Chemother. 33, 1167 (1989). Comparative in vitro antimicrobial spectrum: T. Kojima et al., ibid. 1980. Pharmacokinetics: S. Nakamura et al., ibid. 34, 89 (1990). Subacute toxicity studies: M. Yasuba et al., Chemotherapy 39, Suppl. 4, 180 (1991), C.A. 115, 247561d (1991); M. Iida et al., ibid. 195, C.A. 115, 247562e (1991).

  • Ciprofloxacin CAS Registry Number: 85721-33-1 环丙沙星


    CAS Name: 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acidPercent Composition: C 61.62%, H 5.48%, F 5.73%, N 12.68%, O 14.49%
    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. Antibacterial spectrum in vitro: B. Watt, F. V. Brown, J. Antimicrob. Chemother. 17, 605 (1986); C. M. Bassey et al., ibid. 623. HPLC determn in biological fluids: W. Gau et al., J. Liq. Chromatogr. 8, 485 (1985). Pharmacokinetics: G. Hoffken et al., Antimicrob. Agents Chemother. 27, 375 (1985). Clinical trials: C. A. Ramirez et al., ibid. 28, 128 (1985); B. E. Scully et al., Lancet 1, 819 (1986). Symposia on antibacterial spectrum and clinical use: Am. J. Med. 82, Suppl. 4A, 1-404 (1987); J. Antimicrob. Chemother. 26, Suppl. F, 3-193 (1990). Review of clinical safety and efficacy in children: R. Kubin, Infection 21, 413-421 (1993).

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