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

Lymecycline CAS Registry Number: 992-21-2 四环素亚甲赖氨酸

CAS Name: N6-[[[[(4S,4aS,5aS,6S,12aS)-4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacenyl]carbonyl]amino]methyl]-L-lysine
Additional N...
Literature References: Semi-synthetic antibiotic related to tetracycline, q.v. Prepn: R. K. Blackwood, K. J. Brunings, US 3042716 (1962 to Pfizer); F. Lauria, W. Logemann, DE 1134071 (1962 to Carlo Erba), C.A. 58, 492 (1963); E. Tubaro, E. Raffaldoni, Boll. Chim. Farm. 100, 9 (1961). Clinical pharmacokinetics: A. Schreiner, A. Digranes, Chemotherapy (Basel) 31, 261 (1985). Comparison with doxycycline of phototoxic potential: M. Bjellerup, B. Ljunggren, Br. J. Dermatol. 130, 356 (1994). Clinical trial in acne: L. Bossuyt et al., Eur. J. Dermatol. 13, 130 (2003); of combination with adapalene: W. J. Cunliffe et al., J. Am. Acad. Dermatol. 49, S218 (2003).

Apicycline CAS Registry Number: 15599-51-6 阿哌环素

CAS Name: a-[4-(Dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacenecarboxamido]-4-(2-hydroxyethyl)-1-piperazineacetic acid
Additional Name...
Literature References: Semi-synthetic antibiotic similar to tetracycline. Prepn: Rondelet, NL 6515688 C.A. 66, 46260a (1967) and BE 673130 C.A. 68, 104840u (1968) (both 1966 to Recherche Ind. Ther.); Valcavi et al., Farmaco Ed. Sci. 21, 775 (1966); Rondelet, Froment, Ann. Pharm. Fr. 26, 63 (1968).

Penicillin G Benzhydrylamine CAS Registry Number: 1538-11-0

CAS Name: [2S-(2a,5a,6b)]-3,3-Dimethyl-7-oxo-6-[(phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid compd with a-phenylbenzenemethanamine (1:1)
Additional Names: 1,1-diphen...
Literature References: Semi-synthetic antibiotic. Prepd from potassium penicillin G and benzhydrylamine HCl in dil acetone: Hagemann et al., Ann. Pharm. Fr. 12, 565 (1954); Goldsmith et al., Antibiot. Chemother. 5, 648 (1955); Penau, Hagemann, US 2710863 (1955 to Labs. Français de Chimiothérapie).

Penicillin V Hydrabamine CAS Registry Number: 6591-72-6

Additional Names: N,N'-Bis(dehydroabietyl)ethylenediamine bis(phenoxymethylpenicillin); hydrabamine phenoxymethyl penicillin; hydrabamine penicillin V
Percent Composition: C 68.49%, H 7.77%, N ...
Literature References: Semi-synthetic antibiotic. Prepn: DeRose, US 2812326 (1956 to Abbott).

Penicillin G Hydrabamine CAS Registry Number: 3344-16-9 4-硫-1-氮杂双环[3.2.0]庚烷-2-羧酸,3,3-二甲基-7-氧代-6-[(苯乙酰)氨基]-[2S-(2,5,6)]-,组成 [1R-[1(1R,4aS,10aR*),4a,10a]]-N,N'-双[[1,2,3,4,4a,9,10,10a-辛氢-1,4a-二甲基-7-(

Additional Names: N,N'-Bis(dehydroabietyl)ethylenediamine dipenicillin G; benzylpenicillinic acid N,N'-bis(dehydroabietyl)ethylenediamine double salt; hydrabamine penicillin G
Percent Compositi...
Literature References: Semi-synthetic antibiotic. Prepn: L. C. Cheney, US 2812325 (1957). Pharmacology: D. W. MacCorquodale et al., Antibiot. Annu. 1954-1955, 133; M. H. Lepper, H. W. Spies, ibid. 137; A. F. DeRose et al., Antibiot. Chemother. 5, 315, 324 (1955). Purification: A. F. DeRose, US 2812326 (1957 to Abbott).

Penicillin G Procaine CAS Registry Number: 6130-64-9

CAS Name: (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-[(phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid compd with 2-(diethylamino)ethyl 4-aminobenzoate (1:1) monohydrate
Additional...
Literature References: Semi-synthetic antibiotic. Prepn: N. P. Sullivan et al., Science 107, 169 (1948); C. J. Sullivan et al., J. Am. Chem. Soc. 70, 1287 (1948); H. W. Rhodehamel, Jr., US 2515898 (1950 to Eli Lilly). Crystal structure: Rose, Anal. Chem. 27, 1841 (1955). Toxicity: K. Soehring et al., Arzneim.-Forsch. 1, 28 (1951). Soly profile: P. J. Weiss et al., Antibiot. Chemother. 7, 374 (1957). Pharmacokinetics in horses: S. M. Stover et al., Am. J. Vet. Res. 42, 629 (1981); in humans: B. T. Goh et al., Br. J. Vener. Dis. 60, 371 (1984). Review of use in syphilis: M. W. Adler, Br. Med. J. 288, 551-553 (1984).

Penimepicycline CAS Registry Number: 4599-60-4

CAS Name: (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-[(phenoxyacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid compd with (4S,4aS,5aS,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydr...
Literature References: Semi-synthetic antibiotic. Prepn: Pedrazzoli et al., Boll. Chim. Farm. 98, 516 (1959), C.A. 54, 3856a (1960); Gradnik, Pedrazzoli, GB 897826 (1962 to E.R.A.S.M.E.), C.A. 57, 15034e (1962). Properties: Gradnik et al., Pharm. Acta Helv. 35, 529 (1960).

Irofulven CAS Registry Number: 158440-71-2 (-)-伊洛福芬

CAS Name: (6'R)-6'-Hydroxy-3'-(hydroxymethyl)-2',4',6'-trimethylspiro[cyclopropane-1,5'-[5H]inden]-7'(6'H)-one
Additional Names: (hydroxymethyl)acylfulvene; HMAFPercent Composition: C 73.15%, H...
Literature References: Semi-synthetic antitumor agent derived from illudin S, q.v. Inhibits DNA synthesis and induces apoptosis in tumor cells. Prepn: M. J. Kelner et al., US 5523490 (1996 to Univ. California); T. C. McMorris et al., J. Nat. Prod. 59, 896 (1996). Enantioselective synthesis: idem et al., J. Org. Chem. 69, 619 (2004). Effect on DNA integrity and apoptosis: J. M. Woynarowski et al., Biochem. Pharmacol. 54, 1181 (1997). Clinical pharmacokinetics and toxicology: J. Alexandre et al., Clin. Cancer Res. 10, 3377 (2004). Clinical evaluation in hormone-refractory prostate cancer: N. Senzer et al., Am. J. Clin. Oncol. 28, 36 (2005). Review: M. Baekelandt, Curr. Opin. Invest. Drugs 3, 1517-1526 (2002).

Sulbactam CAS Registry Number: 68373-14-8 舒巴坦酸

CAS Name: (2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide
Additional Names: penicillanic acid sulfone; penicillanic acid 1,1-dioxidePercent Compositio...
Literature References: Semi-synthetic b-lactamase inhibitor. Prepn and use with b-lactam antibiotics: BE 867859; W. E. Barth, US 4234579 (1978, 1980 both to Pfizer); R. A. Volkmann et al., J. Org. Chem. 47, 3344 (1982). b-Lactamase activity and antibacterial spectrum in vitro: A. R. English et al., Antimicrob. Agents Chemother. 14, 414 (1978); R. N. Jones et al., Diagn. Microbiol. Infect. Dis. 3, 489 (1985). HPLC determn in human plasma and urine: J. Haginaka et al., J. Chromatogr. 341, 115 (1985). Pharmacokinetics in humans: G. Foulds et al., Antimicrob. Agents Chemother. 23, 692 (1983). Clinical study of synergistic effect with ampicillin: S. Mehtar et al., J. Antimicrob. Chemother. 17, 389 (1986); B. V. Stromberg et al., Surg. Gynecol. Obstet. 162, 575 (1986). Review of activity and therapeutic use of sulbactam with ampicillin: D. M. Campoli-Richards, R. N. Brogden, Drugs 33, 577-609 (1987).

Clomocycline CAS Registry Number: 1181-54-0 氯莫环素

CAS Name: 7-Chloro-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-N-(hydroxymethyl)-6-methyl-1,11-dioxo-2-naphthacenecarboxamide
Additional Names: chlormethylenecyc...
Literature References: Semi-synthetic broad spectrum antibiotic related to tetracycline, q.v. Prepn: Banci, Tubaro, Boll. Chim. Farm. 102, 471 (1963); BE 628142 (1963 to AB Leo), C.A. 60, 15805f (1964).