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

Colforsin CAS Registry Number: 66575-29-9 佛司可林

CAS Name: (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one
Additional Names: 7b-acetoxy-8,13-epoxy-1...
Literature References: Diterpene isolated from Coleus forskohlii, Briq. Labiatae, possessing vasodilating and cardiostimulatory properties. Isoln and characterization: S. V. Bhat et al., Tetrahedron Lett. 1977, 1669; eidem, DE 2557784; eidem, US 4088659 (1977, 1978 both to Hoechst). Synthesis by hydroxylation of 9-deoxyforskolin: N. J. Hrib, Tetrahedron Lett. 28, 19 (1987); see also F. E. Ziegler et al., J. Am. Chem. Soc. 109, 8115 (1987). Stereocontrolled synthesis of the 3-ring system: S. Hashimoto et al., Chem. Commun. 1987, 24. Total synthesis of (±)-forskolin: S. Hashimoto et al., J. Am. Chem. Soc. 110, 3670 (1988); E. J. Corey et al., ibid. 3672. Positive inotropic and blood-pressure lowering activity: E. Lindner et al., Arzneim.-Forsch. 28, 284 (1978). Activates adenylate cyclase: H. Metzger, E. Lindner, ibid. 31, 1248 (1981). Binds to catalytic site of adenylate cyclase: T. Pfeuffer, H. Metzger, FEBS Lett. 146, 369 (1982). Lowers intraocular pressure: J. Capriolli, M. Sears, Lancet 1, 958 (1983). In treatment of glaucoma: eidem, US 4476140 (1984 to Yale University). Reviews: K. B. Seaman, J. W. Daly, J. Cyclic Nucleotide Res. 1981, 201; K. B. Seaman, "Forskolin and Adenylate Cyclase: New Opportunities in Drug Design" in Annu. Rep. Med. Chem. 19, D. M. Bailey, Ed. (Academic Press, New York, 1984) pp 293-302.

Cafestol CAS Registry Number: 469-83-0 咖啡油醇

CAS Name: [3bS-(3ba,5ab,7b,8b,10aa,10bb)]-3b,4,5,6,7,8,9,10,10a,10b,11,12-Dodecahydro-7-hydroxy-10b-methyl-5a,8-methano-5aH-cyclohepta[5,6]naphtho[2,1-b]furan-7-methanol
Additional Names: cafes...
Literature References: Diterpenoid constituent of coffee. Isoln from green coffee oil: Slotta, Neisser, Ber. 71, 1991, 2342 (1938); C. Djerassi et al., J. Org. Chem. 18, 1449 (1953). Prepn and purification: R. Bertholet, US 4692534 (1987 to Nestec). Structure: C. Djerassi et al., J. Am. Chem. Soc. 81, 2386 (1959); R. A. Finnegan, C. Djerassi, ibid. 82, 4342 (1960). Stereochemical studies: R. A. Finnegan, J. Org. Chem. 26, 3057 (1961); A. I. Scott et al., J. Am. Chem. Soc. 84, 3197 (1962); A. I. Scott et al., Tetrahedron 20, 1339 (1964). Stereospecific total synthesis of (±)-form: E. J. Corey et al., J. Am. Chem. Soc. 109, 4717 (1987).

Taxodione CAS Registry Number: 19026-31-4 落羽松二酮

CAS Name: (4bS-trans)-4b,5,6,7,8,8a-Hexahydro-4-hydroxy-4b,8,8-trimethyl-2-(1-methylethyl)-3,9-phenanthrenedione
Additional Names: 11-hydroxy-13-isopropylpodocarpa-7,9(11),13-triene-6,12-dione<...
Literature References: Diterpenoid quinone methide with tumor-inhibitory properties. Isoln of naturally occurring (+)-form from Taxodium distichum Rich, Taxodiaceae: S. M. Kupchan et al., J. Am. Chem. Soc. 90, 5923 (1968). Structure: eidem, J. Org. Chem. 34, 3912 (1969). Total synthesis of the racemate: K. Mori, M. Matsui, Tetrahedron 26, 3467 (1970); T. Matsumoto et al., Bull. Chem. Soc. Jpn. 44, 2766 (1971); 50, 1575 (1977); D. L. Snitman et al., Tetrahedron Lett. 1979, 2477; R. V. Stevens, G. S. Bisacchi, J. Org. Chem. 47, 2396 (1982). Total synthesis of the (+)-form: T. Matsumoto et al., Bull. Chem. Soc. Jpn. 50, 266 (1977); R. H. Burnell et al., Can. J. Chem. 65, 775 (1987). Antitumor activity studies: Hanson et al., Science 168, 378 (1970).

Triptolide CAS Registry Number: 38748-32-2 雷公藤内酯醇

CAS Name: (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one
Additional N...
Literature References: Diterpenoid triepoxide with immunosuppressant and antitumor properties; isolated from the Chinese medicinal herb, Tripterygium wilfordii Hook. f., Celastraceae. Isoln and structure determn: S. M. Kupchan et al., J. Am. Chem. Soc. 94, 7194 (1972). Synthesis of racemate: R. S. Buckanin et al., ibid. 102, 1200 (1980); of naturally occurring (-)-form: D. Yang et al., ibid. 121, 5579 (1999). HPLC and SPE determn in Tripterygium root extracts: A. M. Brinker, I. Raskin, J. Chromatogr. A 1070, 65 (2005). Animal studies of male antifertility effects: A. P. S. Hikim et al., J. Androl. 21, 431 (2000); P. N. Huynh et al., ibid. 689. Mechanistic studies of apoptotic and antitumor activities: W.-T. Chang et al., J. Biol. Chem. 276, 2221 (2001); T. M. Kiviharju et al., Clin. Cancer Res. 8, 2666 (2002); S. J. Leuenroth, C. M. Crews, Chem. Biol. 12, 1259 (2005). Review of anti-inflammatory and immunosuppressive properties: B. J. Chen, Leuk. Lymphoma 42, 253-265 (2001).

Seyferth-Gilbert Reagent CAS Registry Number: 27491-70-9 (重氮甲基)膦酸二甲酯

CAS Name: (Diazomethyl)phosphonic acid dimethyl ester
Additional Names: dimethyl diazomethylphosphonate
Percent Composition: C 24.01%, H 4.70%, N 18.67%, O 31.98%, P 20.64%
Literature References: Divalent carbon transfer reagent. Prepn: D. Seyferth, R. S. Marmor, Tetrahedron Lett. 11, 2493 (1970); and applications in organophosphorus syntheses: D. Seyferth et al., J. Org. Chem. 36, 1379 (1971). Reactions with aldehydes and aryl ketones to form alkynes: J. C. Gilbert, U. Weerasooriya, ibid. 47, 1837 (1982). Improved prepn: D. G. Brown et al., ibid. 61, 2540 (1996).

Azacitidine CAS Registry Number: 320-67-2 阿扎胞苷

CAS Name: 4-Amino-1-b-D-ribofuranosyl-1,3,5-triazin-2(1H)-one
Additional Names: 5-azacytidine; 5-AzaC; ladakamycinTrademarks: Mylosar (formerly); Vidaza (Pharmion)
Percent Composition: C 39....
Literature References: DNA methylation inhibitor; analog of the pyrimidine nucleoside, cytidine, q.v. Chemical synthesis: A. Piskala, F. Sorm, Collect. Czech. Chem. Commun. 29, 2060 (1964); M. W. Winkley, R. K. Robins, J. Org. Chem. 35, 491 (1970). Production by fermentation of Streptoverticillium ladakanus and activity: L. J. Hanka et al., Antimicrob. Agents Chemother. 1966, 619; M. E. Bergy, R. R. Herr, ibid. 625. HPLC determn in pharmaceutical prepns: L. D. Kissinger, N. L. Stemm, J. Chromatogr. 353, 309 (1986). Toxicology study: P. E. Palm, C. J. Kensler, U.S. Clearinghouse Fed. Sci. Tech. Inform. (PB-194791, 1970) 191 pp., C.A. 75, 33704j (1971). Review of clinical experience in acute nonlymphocytic leukemia: A. B. Glover et al., Cancer Treat. Rep. 71, 737-746 (1987); of mechanism of action: A. B. Glover, B. Leyland-Jones, ibid. 959-964. Review of carcinogenic risk: IARC Monographs 50, 47-63 (1990). Clinical efficacy in b-thalassemia: C. H. Lowrey, A. W. Nienhuis, N. Engl. J. Med. 329, 845 (1993); in myelodysplastic syndrome: L. R. Silverman et al., J. Clin. Oncol. 20, 2429 (2002); A. B. Kornblith et al., ibid. 2441.

Brostallicin CAS Registry Number: 203258-60-0

CAS Name: N-[5-[[[5-[[[2-[(Aminoiminomethyl)amino]ethyl]amino]carbonyl]-1-methyl-1H-pyrrol-3-yl]amino]carbonyl]-1-methyl-1H-pyrrol-3-yl]-4-[[[4-[(2-bromo-1-oxo-2-propenyl)amino]-1-methyl-1H-pyrrol...
Literature References: DNA minor groove binder; bromoacryloyl derivative of distamycin A, q.v. Prepn: P. Cozzi et al., WO 9804524; eidem, US 6482920 (1998, 2002 both to Pharmacia Upjohn). LC/MS/MS determn in plasma: S. Calderoli et al., J. Pharm. Biomed. Anal. 32, 601 (2003). Mechanism of action studies: C. Geroni et al., Cancer Res. 62, 2332 (2002); A. Fedier et al., Br. J. Cancer 89, 1559 (2003). Clinical pharmacokinetics and evaluation in advanced solid tumors: A. J. ten Tije et al., Clin. Cancer Res. 9, 2957 (2003); A. C. Lockhart et al., ibid. 10, 468 (2004). Review of clinical development: M. Broggini et al., Anti-Cancer Drugs 15, 1-6 (2004).

Cidofovir CAS Registry Number: 113852-37-2 西多福韦

CAS Name: [[(1S)-2-(4-Amino-2-oxo-1(2H)-pyrimidinyl)-1-(hydroxymethyl)ethoxy]methyl]phosphonic acid
Additional Names: (S)-1-[3-hydroxy-2-(phosphonylmethoxy)propyl]cytosine; (S)-HPMPCTrademarks:...
Literature References: DNA synthesis inhibitor. Prepn: A. Holy et al., EP 253412; eidem, US 5142051 (1988, 1992 both to Ceskoslov. Akad. Ved; Rega Inst.); and activity vs cytomegalovirus: R. Snoeck et al., Antimicrob. Agents Chemother. 32, 1839 (1988). Syntheses: J. J. Bronson et al., Nucleosides Nucleotides 9, 745 (1990); P. R. Brodfuehrer et al., Tetrahedron Lett. 35, 3243 (1994). Activity vs herpes simplex virus: G. Andrei et al., Eur. J. Clin. Microbiol. Infect. Dis. 11, 143 (1992). Review of pharmacology and clinical studies: M. J. M. Hitchcock et al., Antiviral Chem. Chemother. 7, 115-127 (1996). Review of clinical potential in poxvirus infections: E. De Clercq, Trends Pharmacol. Sci. 23, 456-458 (2002).

Irinotecan CAS Registry Number: 97682-44-5 伊立替康

CAS Name: [1,4'-Bipiperidine]-1'-carboxylic acid (4S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester
Additional Names: 7-ethyl-1...
Literature References: DNA topoisomerase I inhibitor. Semisynthetic derivative of camptothecin, q.v.; de-esterified in vivo to the active metabolite, 7-ethyl-10-hydroxycamptothecin (SN-38). Prepn: JP Kokai 85 19790; T. Miyasaka et al., US 4604463 (1985, 1986 both to Yakult Honsha); S. Sawada et al., Chem. Pharm. Bull. 39, 1446 (1991). Antitumor activity and toxicity data: T. Kunimoto et al., Cancer Res. 47, 5944 (1987). Mechanism of action study: Y. Kawato et al., ibid. 51, 4187 (1991). Clinical trial in colorectal cancer: J. Y. Douillard et al., Lancet 355, 1041 (2000). Review of pharmacology and clinical experience: N. Masuda et al., Crit. Rev. Oncol. Hematol. 24, 3-26 (1996); S. O'Reilly, E. K. Rowinsky, ibid. 47-70; of clinical toxicity: K. Seiter, Expert Opin. Drug Safety 4, 45-53 (2005).

Topotecan CAS Registry Number: 123948-87-8 拓扑替康

CAS Name: (4S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Additional Names: 9-[(dimethylamino)methyl]-10-hydroxy-(20S)-ca...
Literature References: DNA topoisomerase I inhibitor; semisynthetic analog of camptothecin, q.v. Prepn: J. C. Boehm et al., EP 321122; eidem, US 5004758 (1989, 1991 both to SmithKline Beecham); W. D. Kingsbury et al., J. Med. Chem. 34, 98 (1991). HPLC determn in plasma: J. H. Beijnen et al., J. Pharm. Biomed. Anal. 8, 789 (1990). Clinical pharmacology: E. K. Rowinsky et al., J. Clin. Oncol. 10, 647 (1992); and pharmacokinetics: L. J. C. van Warmerdam et al., Cancer Chemother. Pharmacol. 38, 254 (1996). Clinical evaluation in ovarian cancer: A. P. Kudelka et al., J. Clin. Oncol. 14, 1552 (1996); in small cell lung cancer: J. H. Schiller et al., ibid. 2345. Review of clinical toxicity: K. Seiter, Expert Opin. Drug Safety 4, 45-53 (2005).