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

Foscarnet Sodium CAS Registry Number: 63585-09-1 膦甲酸钠

CAS Name: Dihydroxyphosphinecarboxylic acid oxide trisodium salt
Additional Names: trisodium phosphonoformate; trisodium carboxyphosphateTrademarks: Foscavir (AstraZeneca)
Percent Compositio...
Literature References: Inhibits viral DNA polymerase and reverse transcriptase. Prepn: P. Nylén, Ber. 57B, 1023 (1924). Crystal structure: R. R. Naqvi et al., J. Chem. Soc. A 1971, 2751; S. C. Abrahams, Acta Crystallogr. B28, 2886 (1972). Use as antiviral agent: B. F. H. Eriksson et al., DE 2728685; eidem, US 4215113 (1978, 1980 both to Astra). Activity against herpes simplex virus: E. Helgstrand et al., Science 201, 819 (1978); J. M. Reno et al., Antimicrob. Agents Chemother. 13, 188 (1978); S. Alenius et al., Arch. Virol. 60, 197 (1979). Mechanism of inhibition of Epstein-Barr virus replication: A. K. Datta, R. E. Hood, Virology 114, 52 (1981). Preclinical evaluation: B. Oeberg et al., Int. Congr. Ser. - Excerpta Med. 571, 175 (1982). Inhibitory effect on HIV-1 (HTLV-III/LAV) virus replication in vitro: P. S. Sarin et al., Biochem. Pharmacol. 34, 4075 (1985).

Propacetamol CAS Registry Number: 66532-85-2 丙帕他莫

CAS Name: N,N-Diethylglycine 4-(acetylamino)phenyl ester
Additional Names: N,N-diethylglycine ester with 4'-hydroxyacetanilide; 4-acetamidophenyl (diethylamino)acetate
Percent Composition: C...
Literature References: Injectable prodrug of acetaminophen, q.v. Prepn and pharmacology: J. C. Cognacq, BE 854376; idem, US 4127671 (1977, 1978 both to Hexachimie). Clinical comparison with injectable aspirin: R. De Marneffe, L. Mokassa, C. R. Ther. Pharmacol. Clin. 3, 23 (1985). Clinical studies: P. Delacroix et al., Sem. Hop. 61, 2739 (1985); J. Modai, ibid. 62, 587 (1986).

Parecoxib CAS Registry Number: 198470-84-7 帕瑞昔布

CAS Name: N-[[4-(5-Methyl-3-phenyl-4-isoxazolyl)phenyl]sulfonyl]propanamide
Percent Composition: C 61.61%, H 4.90%, N 7.56%, O 17.28%, S 8.66%
Literature References: Injectable prodrug of valdecoxib, q.v., a selective cyclooxygenase-2 (COX-2) inhibitor. Prepn: J. J. Talley et al., WO 9738986; eidem, US 5932598 (1997, 1999 both to Searle); eidem, J. Med. Chem. 43, 1661 (2000). Clinical pharmacokinetics: A. Karim et al., J. Clin. Pharmacol. 41, 1111 (2001). Pharmacological profile: S. S. V. Padi et al., Eur. J. Pharmacol. 491, 69 (2004). Clinical evaluation in post-surgical pain: N. A. Nussmeier et al., Anesthesiology 104, 518 (2006). Comparison of GI effects with ketorolac: R. R. Stoltz et al., Am. J. Gastroenterol. 97, 65 (2002). Review of pharmacology and clinical experience: S. M. Cheer, K. L. Goa, Drugs 61, 1133-1141 (2001).

Ceftizoxime CAS Registry Number: 68401-81-0 头孢唑肟

CAS Name: (6R,7R)-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-imino-4-thiazolyl)glyox...
Literature References: Injectable third generation cephalosporin antibiotic related to cefotaxime, q.v. Exhibits broad spectrum activity and resistance to b-lactamase hydrolysis. Prepn: T. Takaya et al., DE 2810922; eidem, US 4427674 (1978, 1984 both to Fujisawa). In vitro and in vivo antibacterial activity: T. Kamimura et al., Antimicrob. Agents Chemother. 16, 540 (1979). Comparison with other cephalosporins: M. Nishida et al., J. Antibiot. 32, 1319 (1979). Pharmacokinetics: T. Murakawa et al., Antimicrob. Agents Chemother. 17, 157 (1980). Series of articles on metabolism, pharmacology, laboratory evaluation: Arzneim.-Forsch. 30, 1662-1687 (1980). Toxicity and reproduction studies: K. Fukuhara et al., ibid. 1669. Phase I clinical study: N. Nakashima et al., J. Clin. Pharmacol. 21, 388 (1981). Reviews: J. Antimicrob. Chemother. 10, Suppl. C, 1-355 (1982); D. M. Richards, R. C. Heel, Drugs 29, 281-329 (1985).

Ceforanide CAS Registry Number: 60925-61-3 头孢雷特

CAS Name: (6R,7R)-7-[[[2-(Aminomethyl)phenyl]acetyl]amino]-3-[[[1-(carboxymethyl)-1H-tetrazol-5-yl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: (6R...
Literature References: Injectable, semi-synthetic cephalosporin antibiotic. Prepn: M. A. Kaplan et al., DE 2538804; W. J. Gottstein et al., US 4100346, US 4172196 and US 4182863 (1976, 1978, 1979, 1980 all to Bristol-Myers); W. J. Gottstein et al., J. Antibiot. 29, 1226 (1976). Laboratory evaluation: F. Leitner et al., Antimicrob. Agents Chemother. 10, 426 (1976). In vitro susceptibility comparisons: R. N. Jones et al., J. Antibiot. 30, 576, 583 (1977). Comparative tissue distribution: F. H. Lee et al., Antimicrob. Agents Chemother. 19, 625 (1981). Pharmacokinetics: E. H. Estey et al., Clin. Pharmacol. Ther. 30, 396 (1981); S. S. Hawkins et al., ibid. 468. Clinical study: R. J. Wallace et al., Antimicrob. Agents Chemother. 20, 648 (1981).

Loprinone CAS Registry Number: 106730-54-5 奥普力农

CAS Name: 1,2-Dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile
Additional Names: 1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxonicotinonitrile; olprinone
P...
Literature References: Inotropic agent which inhibits cAMP phosphodiesterase. Prepn: M. Yamanaka et al., JP Kokai 86 218589; eidem, US 4751227 (1986, 1988 both to Eisai). Synthesis: M. Yamanaka et al., J. Labelled Compd. Radiopharm. 31, 125 (1992). Pharmacology: M. Tajimi et al., Arch. Pharmacol. 344, 602 (1991). Pharmacokinetics in dogs: Y. Uemura et al., J. Pharm. Pharmacol. 45, 1077 (1993). Review of pharmacology, toxicology and clinical evaluation: M. Endoh, Cardiovasc. Drug Rev. 11, 432-450 (1993).

Ibopamine CAS Registry Number: 66195-31-1 异波帕胺

CAS Name: 2-Methylpropanoic acid 4-[2-(methylamino)ethyl]-1,2-phenylene ester
Additional Names: 4-[2-(methylamino)ethyl]-o-phenylene diisobutyrate; N-methyldopamine diisobutyric ester; 3,4-di-o...
Literature References: Inotropic agent with dopaminergic and adrenergic agonist activities; converted to active metabolite, deoxyepinephrine, q.v. Prepn: C. Casagrande, G. Ferrari, DE 2734678; eidem, US 4218470 (1978, 1980 both to Simes). Pharmacology: G. F. Melloni et al., Curr. Ther. Res. 25, 406 (1979); eidem, ibid. 26, 466 (1979). Series of articles on synthesis, pharmacology, clinical efficacy: Arzneim.-Forsch. 36, 285-408 (1986). Review of pharmacodynamics, pharmacokinetics and therapeutic efficacy: J. M. Henwood, P. A. Todd, Drugs 36, 11-31 (1988). Series of articles on clinical use in congestive heart failure: Cardiology 77, Suppl. 5, 1-95 (1990). Clinical efficacy and safety in heart failure: J. R. Hampton et al., Lancet 349, 971 (1997). Clinical evaluation in diagnosis of glaucoma: G. Marchini et al., J. Ocul. Pharmacol. Ther. 17, 215 (2001); in treatment of ocular hypertony: L. C. Ugahary et al., Am. J. Ophthalmol. 141, 571 (2006).

Cyromazine CAS Registry Number: 66215-27-8 环丙氨嗪

CAS Name: N-Cyclopropyl-1,3,5-triazine-2,4,6-triamine
Additional Names: 2-cyclopropylamino-4,6-diamino-s-triazineTrademarks: Larvadex (Novartis); Neporex (Novartis); Trigard (Syngenta); Vetrazi...
Literature References: Insect growth regulator. Prepn: H. U. Brechbuhler et al., DE 2736876; eidem, US 4225598 (1978, 1980 to Ciba-Geigy). Activity: R. D. Hall, M. C. Foehse, J. Econ. Entomol. 73, 564 (1980); R. J. Hart et al., Aust. Vet. J. 59, 104 (1982).

Haplophytine CAS Registry Number: 16625-20-0

CAS Name: [15(3aS,7R)]-3,4-Didehydro-19-hydroxy-16,17-dimethoxy-1-methyl-15-(2,3,5,6-tetrahydro-11-hydroxy-4-methyl-1,13-dioxo-1H-3a,7-methanopyrrolo[1,2-a][1,3]benzodiazocin-7(4H)-yl)aspidospermi...
Literature References: Insecticidal alkaloid from the Mexican plant Haplophyton cimicidum A. DC., Apocynaceae: Rogers et al., J. Am. Chem. Soc. 74, 1987 (1952); 76, 2819 (1954). Partial structure: Snyder et al., ibid. 80, 3708 (1958). Structure: Rae et al., ibid. 89, 3061 (1967). Crystal structure and absolute config.: Zacharias, Acta Crystallogr. 26B, 1455 (1970). Synthetic approaches: P. Yates, D. A. Schwartz, Can. J. Chem. 61, 509 (1983). Review: Yates et al., J. Am. Chem. Soc. 95, 7842 (1973).

Affinin CAS Registry Number: 25394-57-4 千日菊酰胺

CAS Name: (2E,6Z,8E)-N-(2-Methylpropyl)-2,6,8-decatrienamide
Additional Names: (E,E,Z)-N-isobutyl-2,6,8-decatrienamide; N-isobutyldeca-trans-2-cis-6-trans-8-trienamide; spilanthol
Percent Co...
Literature References: Insecticidal lipid amide isolated from Heliopsis longipes (A. Gray) Blake, Compositae. Isoln and structure: Acree et al., J. Org. Chem. 10, 236, 449 (1945). Identity with spilanthol: Jacobson, Chem. Ind. (London) 1957, 50. Stereochemistry and synthesis: Crombie, Krasinski, ibid. 1962, 983; Crombie et al., J. Chem. Soc. 1963, 4970.