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

Methyl Aminolevulinate CAS Registry Number: 33320-16-0 5-氨基-4-氧代戊酸甲酯

CAS Name: 5-Amino-4-oxopentanoic acid methyl esterPercent Composition: C 49.64%, H 7.64%, N 9.65%, O 33.07%
Literature References: Prodrug of d-aminolevulinic acid, q.v.; induces production of intracellular protoporphyrin IX. Prepn: S. I. Zav'yalov, A. G. Zavozin, Bull. Acad. Sci. USSR Div. Chem. Sci. 36, 1663 (1987). Porphyrin enrichment in solar keratoses: C. Fritsch et al., Photochem. Photobiol. 68, 218 (1998). Clinical trial in photodynamic therapy of basal cell carcinomas: A. M. Soler et al., Br. J. Dermatol. 145, 467 (2001); C. Vinciullo et al., Br. J. Dermatol. 152, 765 (2005); in actinic keratosis: R. M. Szeimies et al., J. Am. Acad. Dermatol. 47, 258 (2002). Review of pharmacology and clinical experience: M. A. A. Siddiqui et al., Am. J. Clin. Dermatol. 5, 127-137 (2004).

Talniflumate CAS Registry Number: 66898-62-2 他尼氟酯

CAS Name: 2-[[3-(Trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid 1,3-dihydro-3-oxo-1-isobenzofuranyl ester
Additional Names: phthalidyl 2-(3-trifluoromethylanilino)nicotinate; phthalidy...
Literature References: Prodrug of niflumic acid, q.v. Prepn: BE 858864 (1978 to Bago), C.A. 89, 109104 (1978); S. Bago, US 4168313 (1979). Synthesis and pharmacologic study: M. Los et al., Farmaco Ed. Sci. 36, 372 (1981). HPLC determn in plasma: D.-J. Jang et al., Biomed. Chromatogr. 19, 32 (2005). Review of clinical development as a mucoregulator: D. Knight, Curr. Opin. Invest. Drugs 5, 557-562 (2004).

Famciclovir CAS Registry Number: 104227-87-4 泛昔洛韦

CAS Name: 2-[2-(2-Amino-9H-purin-9-yl)ethyl]-1,3-propanediol diacetate (ester)
Additional Names: 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurine; FCVTrademarks: Oravir (SKB); Famvir (SKB)...
Literature References: Prodrug of penciclovir, q.v. Prepn: M. R. Harnden, R. L. Jarvest, AU 85 47560; eidem, US 5246937 (1986, 1993 both to Beecham); M. R. Harnden et al., J. Med. Chem. 32, 1738 (1989). HPLC determn in plasma and urine: J. R. McMeekin et al., Anal. Proc. 29, 178 (1992). Review of metabolism and mode of action: R. A. Vere Hodge, Antiviral Chem. Chemother. 4, 67-84 (1993). Series of articles on pharmacology and pharmacokinetics: ibid. Suppl. 1, 37-68 (1993). Review of clinical efficacy in herpes zoster and genital herpes: R. Circelli et al., Antiviral Res. 29, 141-151 (1996).

Fosphenytoin CAS Registry Number: 93390-81-9 磷苯妥英

CAS Name: 5,5-Diphenyl-3-[(phosphonooxy)methyl]-2,4-imidazolidinedione
Additional Names: 3-(hydroxymethyl)-5,5-diphenylhydantoin phosphate ester; (3-phosphoryloxymethyl)phenytoin; prophenytoin<...
Literature References: Prodrug of phenytoin, q.v. Prepn: V. J. Stella, K. B. Sloan, US 4260769 (1981 to INTERx). Series of articles on chemical properties and pharmacokinetics: S. A. Varia et al., J. Pharm. Sci. 73, 1068-1090 (1984). Pharmacology: R. D. Smith et al., Epilepsia 30, Suppl. 2, S15 (1989). Clinical bioavailablilty and pharmacokinetics: B. D. Jamerson et al., ibid. 31, 592 (1990). Series of articles on use in epilepsy: Neurology 46, Suppl. 1, S1-S28 (1996). Clinical trial in epilepsy and neurosurgery: B. J. Wilder et al., Arch. Neurol. 53, 764 (1996).

Ampiroxicam CAS Registry Number: 99464-64-9 安吡昔康

CAS Name: Carbonic acid ethyl 1-[[2-methyl-3-[(2-pyridinylamino)carbonyl]-2H-1,2-benzothiazin-4-yl]oxy]ethyl ester S,S-dioxide
Additional Names: (±)-4-(1-hydroxyethoxy)-2-methyl-N-2-pyridy...
Literature References: Prodrug of piroxicam, q.v. Prepn: A. Marfat, EP 147177; idem, US 4551452 (both 1985 to Pfizer). Clinical pharmacokinetics: F. C. Falkner et al., Xenobiotica 20, 645 (1990). Toxicity study: M. Iijima et al., Oyo Yakuri 43, 1 (1992); C.A. 116, 187689k (1992). Pharmacology: T. J. Carty et al., Agents Actions 39, 157 (1993). Clinical trial in oral postoperative pain: K. Kurita et al., Oral. Ther. Pharmacol. 10, 138 (1991); in rheumatoid arthritis: S. Irimajiri et al., Jpn. J. Inflammation 12, 81 (1992).

Fospropofol CAS Registry Number: 258516-89-1 磷丙泊酚

CAS Name: [2,6-Bis(1-methylethyl)phenoxy]methanol dihydrogen phosphate
Additional Names: phosphono-O-methyl-2,6-diisopropylphenol
Percent Composition: C 54.16%, H 7.34%, O 27.75%, P 10.74%
Literature References: Prodrug of propofol, q.v. Prepn: V. J. Stella et al., WO 0008033; eidem, US 6204257 (2000, 2001 to Univ. Kansas). Clinical pharmacokinetics and pharmacodynamics: J. Fechner et al., Anesthesiology 99, 303 (2003). Clinical evaluation to induce and maintain sedation: eidem, Anesth. Analg. 100, 701 (2005). Clinical comparison with propofol: E. Gibiansky et al., Anesthesiology 103, 718 (2005); M. M. R. Struys et al., ibid. 730. Review: M. D. Krasowski, Curr. Opin. Invest. Drugs 6, 90-98 (2005).

Valpromide CAS Registry Number: 2430-27-5 丙戊酰胺

CAS Name: 2-Propylpentanamide
Additional Names: 2-propylvaleramide; 2-propylpentamide; dipropylacetamide
Trademarks: Depamide (Sanofi)
Percent Composition: C 67.08%, H 11.96%, N 9.78%, O ...
Literature References: Prodrug of valproic acid, q.v. Prepn: E. Fischer, A. Dilthey, Ber. 35, 844 (1902); M. Tiffeneau, Y. Deux, Compt. Rend. 212, 105 (1941). GC determn in plasma: M. Pokrajac et al., Pharm. Acta Helv. 67, 237 (1992). Review of pharmacology and clinical activity: M. Bialer, Clin. Pharmacokinet. 20, 114-122 (1991).

Triethanolamine CAS Registry Number: 102-71-6 三乙醇胺

CAS Name: 2,2',2''-Nitrilotrisethanol
Additional Names: trihydroxytriethylamine; tris(hydroxyethyl)amine; triethylolamine; trolamine
Percent Composition: C 48.30%, H 10.13%, N 9.39%, O 32.17...
Literature References: Produced along with mono- and diethanolamine by ammonolysis of ethylene oxide. See the refs under Ethanolamine. Monograph: E. J. Fischer, Triäthanolamin und andere Alkanolamine (Heidelberg, 4th ed., 1954).

Diethanolamine CAS Registry Number: 111-42-2 二乙醇胺

CAS Name: 2,2'-Iminobisethanol
Additional Names: 2,2'-iminodiethanol; diethylolamine; bis(hydroxyethyl)amine; 2,2'-dihydroxydiethylamine
Percent Composition: C 45.69%, H 10.55%, N 13.32%, O ...
Literature References: Produced along with mono- and triethanolamine by ammonolysis of ethylene oxide. See refs under Ethanolamine. Toxicity study: H. F. Smyth et al., J. Ind. Hyg. Toxicol. 23, 259 (1941).

Penicillin F CAS Registry Number: 118-53-6 (2S,5R,6R)-6-[[(E)-己-3-烯酰基]氨基]-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸

CAS Name: (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-[(1-oxo-3-hexenyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 2-pentenylpenicillin; penicillin I
Percent Compositio...
Literature References: Produced by certain strains of Penicillium chrysogenum and P. notatum. Separation and purification by partition chromatography, cf. monograph by Boon and Carrington in Chemistry of Penicillin (Princeton, 1949). Prepn of cryst penicillin F: Wintersteiner, Adler, US 2485227 (1949 to Squibb).