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

Cefpiramide CAS Registry Number: 70797-11-4 头孢匹胺

CAS Name: (6R,7R)-7-[[(2R)-[[(4-Hydroxy-6-methyl-3-pyridinyl)carbonyl]amino](4-hydroxyphenyl)acetyl]amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-c...
Literature References: Broad spectrum semi-synthetic cephalosporin antibiotic. Prepn: H. Yamada et al., BE 833063; eidem, US 4156724; US 4160087 (1975, 1979, 1979 all to Sumitomo); eidem, JP Kokai 79 119497 (1979 to Sumitomo), C.A. 92, 11042j (1980); I. Isaka et al., JP Kokai 79 30197 (1979 to Yamanouchi), C.A. 91, 57037a (1979); JP Kokai 84 65094 (1984 to Sumitomo), C.A. 101, 110641w (1984). Prepn, NMR data, antibacterial activity: H. Yamada et al., J. Antibiot. 36, 522, 543 (1983). Pharmacokinetics: H. Matsui et al., Antimicrob. Agents Chemother. 22, 213 (1982); K. Sata et al., ibid. 26, 578 (1984). Metabolism: H. Imasaki et al., ibid. 24, 42 (1983). In vitro activity: H. Wexler et al., ibid. 25, 162 (1984); M. A. Pfaller et al., ibid. 368. Comparison with other cephalosporins: N. J. Khan et al., ibid. 26, 585 (1984). Series of articles on in vitro, in vivo activity, determn in body fluids, pharmacokinetics, clinical studies: Chemotherapy (Tokyo) 31, Suppl. 1, 1-842 (1983).

Benfuracarb CAS Registry Number: 82560-54-1 苯并呋喃硫酰氯

CAS Name: N-[[[[(2,3-Dihydro-2,2-dimethyl-7-benzofuranyl)oxy]carbonyl]methylamino]thio]-N-(1-methylethyl)-b-alanine ethyl ester
Additional Names: 2-methyl-4-(1-methylethyl)-7-oxo-8-oxa-3-thia-2...
Literature References: Broad spectrum soil and foliar insecticide; cholinesterase inhibitor. Prepn and insecticidal properties: A. Tanaka et al., BE 890162; T. Goto et al., US 4413005 (1982, 1983 both to Otsuka). Biological activity and field trials: T. Goto et al., Proc. 10th Conf. Int. Congr. Plant Prot. 1, 360 (1983). Absorption and metabolism in plants: A. Tanaka et al., J. Agric. Food Chem. 33, 1049 (1985). Brief review, field trials: P. Cagnieul, Def. Veg. 38, 3-10 (1984).

Cefoperazone CAS Registry Number: 62893-19-0 头孢哌酮

CAS Name: (6R,7R)-7-[[(2R)-[[(4-Ethyl-2,3-dioxo-1-piperazinyl)carbonyl]amino](4-hydroxyphenyl)acetyl]amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-...
Literature References: Broad spectrum third generation cephalosporin antibiotic. Prepn: I. Saikawa et al., BE 837682; eidem, US 4410522 (1976, 1983 both to Toyama); eidem, Yakugaku Zasshi 99, 929 (1979). Stability in aq soln: eidem, ibid. 1207. In vitro activity: M. V. Borobio et al., Antimicrob. Agents Chemother. 17, 129 (1980). Kinetics in rats: J. Fabre et al., Schweiz. Med. Wochenschr. 110, 264 (1980); in humans: A. F. Allaz, ibid. 109, 1999 (1979). Review of pharmacology and therapeutic efficacy: R. N. Brogden et al., Drugs 22, 423-460 (1981). Symposium on clinical studies: ibid. Suppl. 1, 1-124.

Cefotaxime CAS Registry Number: 63527-52-6 头孢噻肟

CAS Name: (6R,7R)-3-[(Acetyloxy)methyl]-7-[[(2Z)-(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: (6R,7R)-7-[2-(2-a...
Literature References: Broad spectrum third generation cephalosporin antibiotic. The name cefotaxime applies to the isomer having a syn-methoxyimino group. Prepn (unspecified stereochemistry): M. Ochiai et al., DE 2556736; eidem, US 4098888 (1976, 1978 both to Takeda); syn-isomer: R. Heymes, A. Lutz, DE 2702501; eidem, US 4152432 (1977, 1979 both to Roussel-UCLAF). Antibacterial activity: R. Wise, Antimicrob. Agents Chemother. 14, 807 (1978); H. W. Van handuyt, M. Pyckavet, ibid. 16, 109 (1979). Human pharmacology: R. Lüthy et al., ibid. 127. Symposia: Drug Ther. Suppl., 1-108 (Jan. 1981); Rev. Infect. Dis. 4, Suppl., S281-S488 (1982); Diagn. Microbiol. Infect. Dis. 2(3), Suppl., 1S-92S (1984); Infection 13, Suppl. 1, S1-S162 (1985). Comprehensive description: F. J. Muhtadi, M. M. A. Hassan, Anal. Profiles Drug Subs. 11, 139-168 (1982). Series of articles on clinical efficacy: J. Antimicrob. Chemother. 26, Suppl. A, 1-83 (1990).

Oxiconazole Nitrate CAS Registry Number: 64211-46-7 硝酸奥昔康唑

CAS Name: (Z)-1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethanone O-[(2,4-dichlorophenyl)methyl]oxime mononitrate
Additional Names: 2',4'-dichloro-2-(imidazol-1-yl)acetophenone O-(2,4-dichlorob...
Literature References: Broad spectrum topical antimycotic agent. Prepn: G. Mixich et al., DE 2657578; eidem, US 4124767 (1977, 1978 both to Siegfried). Stereospecific synthesis of (E)-, (Z)-isomers, 1H NMR study: G. Mixich, K. Thiele, Arzneim.-Forsch. 29, 1510 (1979). GLC determn in plasma: M. Zell, L. Herzfeld, J. Chromatogr. 229, 111 (1982). In vitro and in vivo antifungal activity: A. Polak, Arzneim.-Forsch. 32, 17 (1982). Study of skin, nail penetration: G. Stueltgen, E. Bauer, Mykosen 25, 74 (1982). Comparison of antifungal imidazoles: W. H. Beggs, IRCS Med. Sci. 11, 677 (1983).

Ofloxacin CAS Registry Number: 82419-36-1 氧氟沙星

CAS Name: 9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
Additional Names: ofloxacineTrademarks: Exocin (Allergan); Flobac...
Literature References: Broad spectrum, fluorinated quinolone antibacterial. Prepn: I. Hayakawa et al., EP 47005; eidem, US 4382892 (1982, 1983 both to Daiichi). Total synthesis: H. Egawa et al., Chem. Pharm. Bull. 34, 4098 (1986). Synthesis and activity of optical isomers: S. Atarashi et al., ibid. 35, 1896 (1987). Antibacterial spectrum of racemate: K. Sato et al., Antimicrob. Agents Chemother. 22, 548 (1982). Mechanism of differential activity of enantiomers: I. Morrissey et al., ibid. 40, 1775 (1996). Toxicity data: H. Ohno et al., Chemotherapy (Tokyo) 32, Suppl. 1, 1084 (1984). Pharmacology and clinical efficacy: Infection 14, Suppl. 1, S1-S109 (1986). Symposium on pharmacokinetics and therapeutic use: Scand. J. Infect. Dis. Suppl. 68, 1-69 (1990). Review of antibacterial spectrum, pharmacology, and clinical efficacy: J. P. Monk, D. M. Campoli-Richards, Drugs 33, 346-391 (1987); of mechanism of action: K. Drlica, Curr. Opin. Microbiol. 2, 504-508 (1999).

Cefpodoxime Proxetil CAS Registry Number: 87239-81-4 头孢泊肟酯

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid 1-[[(1-methylethoxy)carbonyl]oxy]ethyl est...
Literature References: Broad spectrum, orally absorbed third generation cephalosporin, ester prodrug of the active free acid metabolite, cefpodoxime. Prepn: H. Nakao et al., EP 49118; eidem, US 4486425 (1982, 1984 both to Sankyo). Prepn, pharmacokinetics and NMR analysis: K. Fujimoto et al., J. Antibiot. 40, 370 (1987). In vitro and in vivo antibacterial activity: Y. Utsui et al., Antimicrob. Agents Chemother. 31, 1085 (1987). In vitro antibacterial spectrum and susceptibility testing of free acid: R. N. Jones, A. L. Barry, ibid. 32, 443 (1988). Series of articles on antibacterial spectrum, pharmacokinetics, toxicology and clinical studies: Chemotherapy (Tokyo) 36, Suppl. 1, 1-1126 (1988). Symposium on pharmacokinetics and clinical efficacy: J. Antimicrob. Chemother. 26, Suppl. E, 1-101 (1990). Review of chemistry, antibacterial activity, toxicity and clinical studies: H. Nakao et al., Sankyo Kenkyusho Nempo 39, 1-44 (1987), C.A. 109, 27503x (1988).

Bemotrizinol CAS Registry Number: 187393-00-6 双乙基己氧基苯酚甲氧基苯三嗪

CAS Name: 2,2'-[6-(4-Methoxyphenyl)-1,3,5-triazine-2,4-diyl]bis[5-[(2-ethylhexyl)oxy]phenol]
Additional Names: 2,4-bis-[4-(2-ethylhexyloxy)-2-hydroxy]phenyl-6-(4-methoxyphenyl)-1,3,5-triazine; ...
Literature References: Broad spectrum, photostable UV-A and UV-B filter in cosmetics and sunscreens. Prepn: D. Hüglin et al., EP 775698; eidem, US 5955060 (1997, 1999 both to Ciba Specialty Chem.). Lack of estrogenic or androgenic activity: J. Ashby et al., Regul. Toxicol. Pharmacol. 34, 287 (2001). Photostabilizing effects on avobenzone and ethylhexyl methoxycinnamate, q.q.v.: E. Chatelain, B. Gabard, Photochem. Photobiol. 74, 401 (2001). Comprehensive review: S. Mongiat et al., Cosmet. Toiletries 118, 47-54 (2003).

Azimsulfuron CAS Registry Number: 120162-55-2 四唑嘧磺隆

CAS Name: N-[[(4,6-Dimethoxy-2-pyrimidinyl)amino]carbonyl]-1-methyl-4-(2-methyl-2H-tetrazol-5-yl)-1H-pyrazole-5-sulfonamide
Additional Names: 1-(4,6-dimethoxypyrimidin-2-yl)-3-[1-methyl-4-(2-me...
Literature References: Broad spectrum, post-emergent sulfonylurea herbicide which inhibits acetolactate synthase. Prepn: G. Levitt, US 4746353 (1988 to Du Pont). Description of chemical properties and biological activities: T. Marquez et al., Brighton Crop Prot. Conf. - Weeds 1995, 65. Environmental fate: A. C. Barefoot et al., ibid. 713. Absorption, translocation and metabolism: S. Shirakura et al., Weed Res. Jpn. 40, 299 (1995). Efficacy in combination with bensulfuron methyl: eidem, ibid. 29.

Methacycline CAS Registry Number: 914-00-1 甲烯土霉素

CAS Name: [4S-(4a,4aa,5a,5aa,12aa)]-4-Dimethylamino-1,4,4a,5,5a,6,11,12a-octahydro-3,5,10,12,12a-pentahydroxy-6-methylene-1,11-dioxo-2-naphthacenecarboxamide
Additional Names: 6-methyleneoxytet...
Literature References: Broad spectrum, semi-synthetic antibiotic related to tetracycline, q.v. Prepn from oxytetracycline, q.v.: R. K. Blackwood et al., US 2984686 (1961 to Pfizer); eidem, J. Am. Chem. Soc. 83, 2773 (1961); 85, 3943 (1963). Solubility data: J. R. Marsh, P. J. Weiss, J. Assoc. Off. Anal. Chem. 50, 257 (1967). Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Comparative clinical study with ampicillin, q.v., in chronic bronchitis: S. Chodosh et al., Chest 69, 587 (1976).