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

Polifeprosan CAS Registry Number: 90409-78-2 聚苯丙生

CAS Name: Decanedioic acid polymer with 4,4'-[1,3-propanediylbis(oxy)]bis[benzoic acid]
Additional Names: 1,3-bis(p-carboxyphenoxy)propane-sebacic acid copolymer; poly[1,3-bis(p-carboxyphenoxy)...
Literature References: Biodegradable, hydrophobic polymers developed for use as implantable drug delivery systems. Prepn of various copolymers: K. W. Leong et al., Polym. Prepr. 25, 201 (1984); eidem, J. Biomed. Mater. Res. 19, 941 (1985). Toxicology and biocompatibility studies: C. T. Laurencin et al., Clin. Lab. Med. 10, 549 (1990). Review of polymer design, synthesis and physical properties: J. Tamada, R. Langer, J. Biomater. Sci. Polym. Ed. 3, 315-353 (1992).

Octyl Cyanoacrylate CAS Registry Number: 6701-17-3 奥克立酯

CAS Name: 2-Cyano-2-propenoic acid octyl ester
Additional Names: ocrilate; ocrylate; n-octyl a-cyanoacrylate; capryl a-cyanoacrylate; octyl 2-cyanoacrylate
Trademarks: Dermabond (Ethicon); N...
Literature References: Biodegradable, topical surgical glue; upon contact with tissue anions, monomer rapidly polymerizes to form a strong adhesive. Preparative method: A. E. Ardis, US 2467927 (1949 to B. F. Goodrich). Prepn, polymerization and degradation: F. Leonard et al., J. Appl. Polym. Sci. 10, 259 (1966). Biocompatibility, histomorphology, and clinical characteristics: A. Nitsch et al., Aesth. Plast. Surg. 29, 53 (2005). Clinical trial for closure of lacerations: J. Quinn et al, J. Am. Med. Assoc. 277, 1527 (1997); of lacerations and incisions: A. J. Singer et al., Surgery 131, 270 (2002); for repair of inguinal hernia: G. Miyano et al., J. Pediatr. Surg. 39, 1867 (2004).

Dinosterol CAS Registry Number: 58670-63-6 甲藻甾醇

CAS Name: (3b,4a,5a,22E)-4,23-Dimethylergost-22-en-3-ol
Additional Names: 4a-methyl-5a(H)-D22-23,24-dimethylcholesten-3b-ol; Black Sea sterol
Percent Composition: C 84.04%, H 12.23%, O 3.73%
Literature References: Biogenetically important marine sterol isolated from the toxic dinoflagellate, Gonyaulax tamarensis. Isoln and structure determn: Y. Shimizu et al., J. Am. Chem. Soc. 98, 1059 (1976). Stereochemistry: J. Finer et al., J. Org. Chem. 43, 1990 (1978). Identity with the Black Sea sterol: J. J. Boon et al., Nature 277, 125 (1979). Stereospecific synthesis: A. Y. L. Shu, C. Djerassi, Tetrahedron Lett. 22, 4627 (1981).

Cadaverine CAS Registry Number: 462-94-2 1,5-二氨基戊烷

CAS Name: 1,5-Pentanediamine
Additional Names: pentamethylenediamine; animal coniine
Percent Composition: C 58.77%, H 13.81%, N 27.42%
Literature References: Biogenic polyamine and homolog of putrescine, q.v., produced by decarboxylation of lysine. Found in cholera discharge. Isoln: Bocklisch, Ber. 18, 1922 (1885); Ackermann, Z. Physiol. Chem. 54, 16 (1907). Prepn: Ladenburg, Ber. 18, 2956 (1885). GC determn in foods: W. F. Staruszkiewicz, J. F. Bond, J. Assoc. Off. Anal. Chem. 64, 584 (1981). Metabolism study of 14C-cadaverine in rat brain: S. K. Salzman, M. Stepita-Klauco, J. Neurochem. 37, 1308 (1981). Biosynthetic study in S. ruminantium: Y. Kamio et al., J. Biol. Chem. 257, 3326 (1982).

Virulizin® (Lorus) CAS Registry Number: 216586-46-8

Additional Names: Virulizin-2g
Literature References: Biological response modifier extracted from bovine bile. Prepn: R. Rang, WO 9507089 (1995 to Imutec); idem, US 6551623 (2003 to Lorus). In vivo antitumor activity: N. Feng et al., Cancer Chemother. Pharmacol. 51, 247 (2003). Clinical evaluation in pancreatic cancer: E. Warner et al., Clin. Invest. Med. 17, 37 (1994). Mechanism of action studies: M. Y. Cao et al., Cancer Immunol. Immunother. 54, 229 (2005); H. Li et al., ibid. 1115. Review of pharmacology and therapeutic potential: E. S. Ferdinandi et al., Expert Opin. Invest. Drugs 8, 1721-1735 (1999).

Levamisole CAS Registry Number: 14769-73-4 左旋咪唑

CAS Name: (6S)-2,3,5,6-Tetrahydro-6-phenylimidazo[2,1-b]thiazole
Additional Names: (-)-6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole
Trademarks: Levovermax (Virbac); Totalon (Mallinckrod...
Literature References: Biological response modifier with anthelmintic activity. Prepn of racemate: A. H. M. Raeymaekers et al., US 3274209 (1966 to Janssen); eidem, J. Med. Chem. 9, 545 (1966). Pharmacology: D. Thienpoint et al., Nature 209, 1084 (1966). Prepn and abs config of isomers: A. H. M. Raeymaekers et al., Tetrahedron Lett. 1967, 1467. See also: M. W. Bullock et al., J. Med. Chem. 11, 169 (1968); US 3565907 (1971 to Am. Cyanamid); Dewar et al., US 3579530 (1971 to ICI). Stereospecific inhibition of succinic dehydrogenase: H. Van den Bossche, P. A. J. Janssen, Biochem. Pharmacol. 18, 35 (1969). Exptl effect on IL-1 production: E. S. Kimball, Ann. N.Y. Acad. Sci. 685, 259 (1993). Review of pharmacology: H. Schneiden, Int. J. Immunopharmacol. 3, 9 (1981); of clinical use in parasitic infections: M. J. Miller, Drugs 20, 122-130 (1980). Determn in animal tissues by ELISA: J. J. Silverlight, R. Jackman: Analyst 119, 2705 (1994); by LC-MS: A. Cannavan et al., ibid. 120, 331 (1995). Clinical trial with fluorouracil in colon cancer: C. G. Moertel et al., Ann. Intern. Med. 122, 321 (1995). Review of immunopharmacology and clinical trials in cancer treatment: H. C. Stevenson et al., J. Clin. Oncol. 9, 2052-2066 (1991); M. De Brabander et al., Anticancer Res. 12, 177-188 (1992); W. K. Amery, J. P. Bruynseels, Int. J. Immunopharmacol. 14, 481-486 (1992).

Bropirimine CAS Registry Number: 56741-95-8 溴匹立明

CAS Name: 2-Amino-5-bromo-6-phenyl-4(1H)-pyrimidinone
Additional Names: 5-bromo-6-phenylisocytosine; 5-bromo-2,3-dihydro-2-imino-6-phenyl-4[1H]-pyrimidinone; ABPPTrademarks: Remisar (Pharmacia ...
Literature References: Biological response modifier; induces production of a-interferon. Prepn: T. B. Brown, M. F. G. Stevens, J. Chem. Soc. Perkin Trans. 1 1975, 1023; M. F. G. Stevens et al., Anti-Cancer Drug Des. 10, 215 (1995). Antiviral and interferon-inducing effects: D. A. Stringfellow et al., J. Interferon Res. 1, 1 (1980). Structure-activity study: H. I. Skulnick et al., J. Med. Chem. 28, 1864 (1985). Crystal structure and 1H-NMR: M. F. G. Stevens et al., Anti-Cancer Drug Des. 10, 203 (1995). Review of clinical studies in bladder cancer: M. F. Sarosdy, Ann. N.Y. Acad. Sci. 685, 301-308 (1993).

Chromium Picolinate CAS Registry Number: 14639-25-9 吡啶甲酸铬

CAS Name: Tris(2-pyridinecarboxylato-N1,O2)chromium
Additional Names: chromium tripicolinate; chromium(III) trispicolinate
Trademarks: Chromax (Nutrition 21)
Percent Composition: C 51.68%...
Literature References: Biologically active form of chromium. General prepn, chemical and biological properties: G. W. Evans, D. J. Pouchnik, J. Inorg. Biochem. 49, 177 (1993). Clinical effect on insulin metabolism: G. W. Evans, Int. J. Biosocial Med. Res. 11, 163 (1989). Clinical evaluation of lipid-lowering activity: R. I. Press et al., West. J. Med. 152, 41 (1990). Clinical pharmacokinetics: M. L. Gargas et al., Drug Metab. Dispos. 22, 522 (1994). Use as veterinary diet supplement: M. D. Lindemann et al., J. Anim. Sci. 73, 457 (1995). Review of clinical pharmacology: M. F. McCarty, J. Appl. Nutr. 43, 58-66 (1991); idem, J. Optim. Nutr. 2, 36-53 (1993); of safety studies: T. O. Berner et al., Food Chem. Toxicol. 42, 1029-1042 (2004).

Etonogestrel CAS Registry Number: 54048-10-1 依托孕烯

CAS Name: (17a)-13-Ethyl-17-hydroxy-11-methylene-18,19-dinorpregn-4-en-20-yn-3-one
Additional Names: 17-ethynyl-17b-hydroxy-18-methyl-11-methyleneestr-4-en-3-one; 3-ketodesogestrel; 3-oxodesoge...
Literature References: Biologically active metabolite of desogestrel, q.v.. Prepn: H. Hofmeister et al., EP 51762; eidem, US 4371529 (1982, 1983 both to Schering AG); H. Gao et al., Steroids 62, 398 (1997). Series of articles on clinical experience: Contraception 58, Suppl. 1, 75S-115S (1998). Clinical safety and efficacy: H. B. Croxatto et al., Hum. Reprod. 14, 976 (1999). Review of clinical studies: J. E. Edwards, A. Moore, Br. J. Fam. Plann. 24, 3-16 (1999).

Tirapazamine CAS Registry Number: 27314-97-2 替拉扎明

CAS Name: 1,2,4-Benzotriazin-3-amine 1,4-dioxide
Additional Names: 3-amino-1,2,4-benzotriazine 1,4-dioxideTrademarks: Tirazone (Sanofi Winthrop)
Percent Composition: C 47.19%, H 3.39%, N 31....
Literature References: Bioreductive anticancer agent; selectively toxic to cells under hypoxic conditions. Prepn: R. F. Robbins, K. Schofield, J. Chem. Soc. 1957, 3186; J. C. Mason, G. Tennant, J. Chem. Soc. B 1970, 911. See also: K. Ley et al., DE 2204574; eidem, US 3868371 (1973, 1975 both to Bayer). HPLC determn in plasma: H. Robin, Jr. et al., Cancer Chemother. Pharmacol. 36, 266 (1995). Review of pharmacology and mechanism of action studies: J. M. Brown, Br. J. Cancer 67, 1163-1170 (1993). Clinical evaluation in combination with cisplatin: C. A. Johnson et al., J. Clin. Oncol. 15, 773 (1997).