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

Ciclopirox CAS Registry Number: 29342-05-0 环吡酮胺

CAS Name: 6-Cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridinone
Percent Composition: C 69.54%, H 8.27%, N 6.76%, O 15.44%
Literature References: Broad spectrum antimycotic agent with some antibacterial activity. Prepn: G. Lohaus, W. Dittmar, ZA 6906039; eidem, US 3883545 (1970, 1975 both to Hoechst). In vitro study: eidem, Arzneim.-Forsch. 23, 670 (1973). Series of articles on pharmacokinetics, pharmacology, teratology, toxicity studies: Oyo Yakuri 9, 57-115 (1975), C.A. 83, 53159d, 53538b, 53539c, 71844c, 90833q (1975). Series of articles on chemistry, mechanism of action, toxicology, clinical trials: Arzneim.-Forsch. 31, 1309-1386 (1981). Toxicity data: H. G. Alpermann, E. Schutz, ibid. 1328. Review: S. G. Jue et al., Drugs 29, 330-341 (1985). Review of clinical experience in seborrheic dermatitis: A. Starova, R. Aly, Expert Opin. Drug Saf. 4, 235-239 (2005).

Fenticonazole CAS Registry Number: 72479-26-6 芬替康唑

CAS Name: 1-[2-(2,4-Dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H-imidazole
Additional Names: 1-[2,4-dichloro-b-[[p-(phenylthio)benzyl]oxy]phenethyl]imidazole; 1-(2,4-dichloropheny...
Literature References: Broad spectrum antimycotic; also active as antibacterial. Prepn: D. Nardi et al., DE 2917244; eidem, US 4221803 (1979, 1980 both to Recordati); eidem, Arzneim.-Forsch. 31, 2123 (1981). Series of articles on physico-chemical properties, in vitro and in vivo antibacterial and antifungal activity, pharmacology and toxicology: ibid. 2127-2154. Toxicity data: G. Graziani et al., ibid. 2145. Preliminary clinical comparison with miconazole in vaginal candidiasis: A. Gastaldi, Curr. Ther. Res. 38, 489 (1985). Comparative clinical trials in dermatomycoses: A. Finzi et al., Mykosen 29, 41 (1986); E. M. Kokoschka et al., ibid. 45.

Nitazoxanide CAS Registry Number: 55981-09-4 硝唑尼特

CAS Name: 2-(Acetyloxy)-N-(5-nitro-2-thiazolyl)benzamide
Additional Names: N-(5-nitro-2-thiazolyl)salicylamide acetate (ester); 2-(2'-acetoxy)benzamido-5-nitrothiazoleTrademarks: Alinia (Romark...
Literature References: Broad spectrum antiparasitic agent; inhibits pyruvate ferredoxin oxidoreductase. Prepn: J. F. Rossignol, R. Cavier, DE 2438037; eidem, US 3950351 (1975, 1976 both to S.P.R.L. Phavic); and antiparasitic activity: R. Cavier et al., Eur. J. Med. Chem. - Chim. Ther. 13, 539 (1978). Antibacterial spectrum in vitro: L Dubreuil et al., Antimicrob. Agents Chemother. 40, 2266 (1996). Toxicology: J. R. Murphy, J.-C. Friedmann, J. Appl. Toxicol. 5, 49 (1985). Clinical pharmacokinetics: A. Stockis et al., Int. J. Clin. Pharmacol. Ther. 34, 349 (1996). Clinical trial in intestinal protozoan and helminthic infections: H. Abaza et al., Curr. Ther. Res. 59, 116 (1998). Review of mechanism of action and clinical experience: H. M. Gilles, P. S. Hoffman, Trends Parasitol. 18, 95-97 (2002).

Boscalid CAS Registry Number: 188425-85-6 啶酰菌胺

CAS Name: 2-Chloro-N-(4'-chloro[1,1'-biphenyl]-2-yl)-3-pyridinecarboxamide
Additional Names: 2-chloro-N-(4'-chlorobiphenyl-2-yl)nicotinamide; nicobifenTrademarks: Cantus (BASF); Endura (BASF) Literature References: Broad spectrum carboxamide fungicide used to control diseases in turf, field, row, orchard, and vineyard crops. Prepn: K. Eicken et al., EP 545099; eidem, US 5589493 (1993, 1996 both to BASF). Terrestrial field dissipation study: S. H. Jackson, Pest Manage. Sci. 60, 8 (2003). Comparative field trial vs sclerotinia drop in lettuce: M. E. Matheron, M. Porchas, Plant Dis. 88, 665 (2004). Review of chemistry and toxicology: Boscalid Pesticide Fact Sheet (U.S. EPA, July 2003) 18 pp.

Cefclidin CAS Registry Number: 105239-91-6 1-氨基双环[2.2.2]辛烷,4-(氨基羰基)-1-[[(6R,7R)-7-[[(2Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-(甲氧基亚基)乙酰]-2-羧基-8-羟基-5-呻-1-阿氮双环[4.2.0]辛-2-烯-3-基]甲基]-,内盐

CAS Name: 4-(Aminocarbonyl)-1-[[(6R,7R)-7-[[(2Z)-(5-amino-1,2,4-thiadiazol-3-yl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-azoniabicyclo[2.2.2]oc...
Literature References: Broad spectrum fourth generation cephalosporin antibiotic. Prepn: H. Yamauchi et al., EP 188255; eidem, US 4748171 (1986, 1988 both to Eisai). Structure activity study: I. Sugiyama et al., J. Antibiot. 45, 103 (1992). Comparative in vitro antibacterial spectrum and b-lactamase resistance: N.-A. Watanabe et al., Antimicrob. Agents Chemother. 32, 693 (1988). In vivo antipseudomonal activity: T. Toyosawa et al., Chemotherapy (Tokyo) 42, 1242 (1994). Clinical pharmacokinetics: M. Nakashima et al., J. Clin. Pharmacol. 29, 144 (1989). Toxicity study: K. Ogura et al., Chemotherapy (Tokyo) 40, Suppl. 4, 95 (1992).

Tigecycline CAS Registry Number: 220620-09-7 替加环素

CAS Name: (4S,4aS,5aR,12aS)-4,7-Bis(dimethylamino)-9-[[[(1,1-dimethylethyl)amino]acetyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide
Additi...
Literature References: Broad spectrum glycylcycline antibiotic; semisynthetic tetracycline analogue. Prepn: J. J. Hlavka et al., EP 536515; eidem, US 5494903 (1993, 1996 both to Am. Cyanamid); P.-E. Sum, P. Petersen, Bioorg. Med. Chem. Lett. 9, 1459 (1999). In vivo pharmacodynamics: M. L. van Ogtrop et al., Antimicrob. Agents Chemother. 44, 943 (2000). In vitro activity vs clinical bacterial isolates: A. C. Gales, R. N. Jones, Diagn. Microbiol. Infect. Dis. 36, 19 (2000); D. Milatovic et al., Antimicrob. Agents Chemother. 47, 400 (2003). Mode of action study: G. Bauer et al., J. Antimicrob. Chemother. 53, 592 (2004). Clinical pharmacology: A. K. Meagher et al., Diagn. Microbiol. Infect. Dis. 52, 165 (2005). Clinical evaluation in complicated skin and skin-structure infections: R. G. Postier et al., Clin. Ther. 26, 704 (2004); E. J. Ellis-Grosse et al., Clin. Infect. Dis. 41, S341 (2005); in complicated intra-abdominal infections: T. Babinchak et al., ibid. S354. Review of chemistry, pharmacology and clinical development: E. Rubinstein, D. Vaughan, Drugs 65, 1317-1336 (2005); R. A. Squires, R. G. Postier, Expert Opin. Invest. Drugs 15, 155-162 (2006).

Cefbuperazone CAS Registry Number: 76610-84-9 头孢拉宗

CAS Name: (6R,7S)-7-[[(2R,3S)-2-[[(4-Ethyl-2,3-dioxo-1-piperazinyl)carbonyl]amino]-3-hydroxy-1-oxobutyl]amino]-7-methoxy-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0...
Literature References: Broad spectrum injectable cephamycin. Prepn: I. Saikawa et al., BE 879217; eidem, US 4263292 (1980, 1981 both to Toyama). Distribution of 14C-cefbuperazone in mice: eidem, Jpn. J. Antibiot. 35, 2159 (1982), C.A. 98, 11062w (1982). In vitro and in vivo antibacterial activity: M. Tai et al., Antimicrob. Agents Chemother. 22, 728 (1982). General pharmacology: A. Takai et al., Jpn. J. Antibiot. 35, 2139 (1982), C.A. 98, 65142r (1982). Absorption, distribution, excretion: I. Saikawa et al., ibid. 2163, C.A. 98, 100691t (1982). Series of articles on cefbuperazone: Chemotherapy (Tokyo) 30, Suppl. 3 (1982) 986 pp. Stability and degradation studies: S. Takano et al., Yakugaku Zasshi 103, 62 (1983).

Netilmicin CAS Registry Number: 56391-56-1 奈替米星

CAS Name: O-3-Deoxy-4-C-methyl-3-(methylamino)-b-L-arabinopyranosyl-(1®6)-O-[2,6-diamino-2,3,4,6-tetradeoxy-a-D-glycero-hex-4-enopyranosyl-(1®4)]-2-deoxy-N1-ethyl-D-streptamine
Additional Names...
Literature References: Broad spectrum semi-synthetic aminoglycoside antibiotic, related to sisomicin, q.v. Prepn: M. J. Weinstein et al., DE 2437160 (1975 to Sherico); J. J. Wright, US 4029882 (1977 to Schering); J. J. Wright et al., US 4002742 (1977 to Schering). Structure and synthesis: J. J. Wright, Chem. Commun. 1976, 206. Biological activity: G. H. Miller et al., Antimicrob. Agents Chemother. 10, 827 (1976). Radioimmunoassay: A. Broughton et al., Clin. Chem. 24, 717 (1978). Pharmacology: W. Raab, Adv. Clin. Pharmacol. 15, 91 (1978); I. Trestman et al., Antimicrob. Agents Chemother. 13, 832 (1978). Metabolism and pharmacokinetics: J. C. Pechere et al., Clin. Pharmacol. Ther. 23, 677 (1978); R. E. Brummett et al., Arch. Otolaryngol. 104, 579 (1978). Clinical studies: J. Klastersky et al., Antimicrob. Agents Chemother. 12, 503 (1977); A. P. Panwalker et al., ibid. 13, 170 (1978). Toxicity studies: L. Albiero et al., Arch. Int. Pharmacodyn. Ther. 233, 343 (1978); F. C. Lust, J. Int. Med. Res. 6, 286 (1978). Review: P. Noone, Drugs 27, 548-578 (1984).

Piperacillin CAS Registry Number: 61477-96-1 哌拉西林

CAS Name: (2S,5R,6R)-6-[[(2R)-[[(4-Ethyl-2,3-dioxo-1-piperazinyl)carbonyl]amino]phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: (2S,...
Literature References: Broad spectrum semi-synthetic antibiotic related to pencillin. Prepn: I. Saikawa et al., DE 2519400; eidem, US 4087424 (1976, 1978 both to Toyama). In vitro studies: G. P. Bodey, B. LeBlanc, Antimicrob. Agents Chemother. 14, 78 (1978); R. Wise et al., ibid. 549. In vitro and in vivo: N. A. Kuck, G. S. Redin, J. Antibiot. 31, 1175 (1978). Pharmacokinetics: M. A. Evans et al., J. Antimicrob. Chemother. 4, 255 (1978). Metabolism: K. Iida et al., Antimicrob. Agents Chemother. 14, 257 (1978). Clinical study: T. Saito, Y. Yamada, Jpn. J. Antibiot. 30, 835 (1977). Toxicity study: A. Takai et al., Chemotherapy (Tokyo) 25, 816 (1977). Review of antibacterial activity, pharmacokinetics: G. L. Mandell, Clin. Ther. 7, Suppl. B, 28-35 (1985). Review of clinical experience in urinary tract infections: S. J. Childs, ibid. 36-45. Series of articles on antibacterial activity and clinical use: Chemotherapy (Tokyo) 36, Suppl. 7, 1-85 (1988).

Ticarcillin CAS Registry Number: 34787-01-4 替卡西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Carboxy-3-thienylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: N-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-az...
Literature References: Broad spectrum semi-synthetic antibiotic related to penicillin. Prepn: BE 646991; E. G. Brain, J. H. Nayler, US 3282926 (1964, 1966 to Beecham Group Ltd.). In vitro studies: H. C. Neu, E. B. Winshell, Antimicrob. Agents Chemother. 1970, 385; R. Sutherland et al., ibid. 390; N. J. Legakis, J. Papavassiliou, J. Antibiot. 28, 912 (1975). In vivo studies: P. Acred et al., Antimicrob. Agents Chemother. 1970, 396. Absorption and excretion: R. Sutherland, P. J. Wise, ibid. 402. Clinical pharmacology: V. Rodriguez et al., Antimicrob. Agents Chemother. 4, 31 (1973); R. D. Libke et al., Clin. Pharmacol. Ther. 17, 441 (1975). Review of pharmacology and therapeutic efficacy: R. N. Brogden et al., Drugs 20, 325-352 (1980).