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

Xanthyletin CAS Registry Number: 553-19-5 花椒树皮素甲

CAS Name: 8,8-Dimethyl-2H,8H-benzo[1,2-b:5,4-b']dipyran-2-one
Additional Names: 7-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-acrylic acid d-lactone; 2,2-dimethylchromenocoumarin
Percent Composit...
Literature References: Linear pyranocoumarin found in Xanthoxylum americanum Mill., Luvanga scandens Ham., Citrus acida Roxb., Rutaceae; Chloroxylon swietenia DC., Meliaceae. Isoln: Bell, Robertson, J. Chem. Soc. 1936, 1828; Bell et al., ibid. 1937, 1542; Späth et al., Ber. 72, 1450 (1939); Bose, Mookerjee, J. Indian Chem. Soc. 21, 181 (1944); Mookerjee, ibid. 23, 41 (1946); King et al., J. Chem. Soc. 1954, 1392. Synthesis: Späth, Hillel, Ber. 72, 2093 (1939); Steck, Can. J. Chem. 49, 2297 (1971); P. Waykole et al., Indian J. Chem. 19B, 238 (1980); V. K. Ahluwalia et al., Monatsh. Chem. 112, 119 (1981); J. Banerji et al., Indian J. Chem. 21B, 496 (1982).

Piritrexim CAS Registry Number: 72732-56-0 吡曲克辛

CAS Name: 6-[(2,5-Dimethoxyphenyl)methyl]-5-methylpyrido[2,3-d]pyrimidine-2,4-diamine
Additional Names: 2,4-diamino-6-(2,5-dimethoxybenzyl)-5-methylpyrido[2,3-d]pyrimidinePercent Composition: C...
Literature References: Lipid soluble dihydrofolate reductase inhibitor. Prepn: E. M. Grivsky et al., J. Med. Chem. 23, 327 (1980); E. M. Grivsky et al., EP 21292 (1981 to Wellcome); E. M. Grivsky, US 4959474 (1990 to Burroughs Wellcome). Biochemistry and antitumor activity: D. S. Duch et al., Cancer Res. 42, 3987 (1982). Cytotoxicity: I. W. Taylor et al., ibid. 45, 978 (1985). Pharmacology and toxicology: C. W. Sigel et al., NCI Monogr. 5, 111 (1987). Antipneumocystis and antitoxoplasma activities: J. A. Kovacs et al., Antimicrob. Agents Chemother. 32, 430 (1988). HPLC determn in plasma: R. G. Foss, C. W. Sigel, J. Pharm. Sci. 71, 1176 (1982). Determn by protein binding assay in plasma: J. L. Woolley, Jr., et al., ibid. 78, 749 (1989). Crystal structure and conformational analysis: P. A. Sutton, V. Cody, J. Am. Chem. Soc. 110, 6219 (1988). Clinical pharmacology in children: P. C. Adamson et al., Cancer Res. 50, 4464 (1990). Clinical evaluation in lung cancer: M. G. Kris et al., Cancer Treat. Rep. 71, 763 (1987); in advanced squamous head and neck cancer: W.-C. Uen et al., Cancer 69, 1008 (1992).

Iofetamine 123 I CAS Registry Number: 75917-92-9 (+-)-4-(碘-123I)-alpha-甲基-N-(1-甲基乙基)-苯乙胺

CAS Name: 4-(Iodo-123I)-a-methyl-N-(1-methylethyl)benzeneethanamine
Additional Names: (±)-p-iodo-123I-N-isopropyl-a-methylphenethylamine; [123I](±)-N-isopropyl-p-iodoamphetamine
Literature References: Lipid soluble radioactive brain imaging agent. Prepn: R. M. Baldwin et al., EP 11858 (1980 to Hoffmann-La Roche); eidem, US 4360511 (1982 to Medi-Physics). Detailed synthesis: L. Carlsen, K. Andresen, Eur. J. Nucl. Med. 7, 280 (1982). Modified synthesis for improved yields: A. Najafi, J. Labelled Compd. Radiopharm. 24, 1167 (1987). Preparative HPLC purification: J. Mertens et al., Nucl. Med. Commun. 5, 705 (1984). Brain uptake and localization: H. S. Winchell et al., J. Nucl. Med. 21, 940 (1980); H. S. Winchell et al., ibid. 947. Distribution kinetics in animals: P. Som et al., Int. J. Nucl. Med. Biol. 12, 185 (1985); in humans: B. L. Holman et al., J. Nucl. Med. 25, 25 (1984). Diagnostic use for cerebral function in Alzheimer's disease: K. A. Johnson et al., Arch. Neurol. 45, 392 (1988). Reviews of radiopharmaceutical production and diagnostic use with single photon emission computed tomography (SPECT) imaging: M. B. Cohen et al., Appl. Radiat. Isot. 37, 749-763 (1986); of diagnostic applications in stroke: C. H. Park et al., RadioGraphics 8, 305-326 (1988); of metabolism and kinetics: R. M. Baldwin, J.-L. Wu, J. Nucl. Med. 29, 122-124 (1988).

Trimetrexate CAS Registry Number: 52128-35-5 三甲曲沙

CAS Name: 5-Methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-2,4-quinazolinediamine
Additional Names: 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline; TMQPercent Composition...
Literature References: Lipophilic dihydrofolate reductase inhibitor structurally related to methotrexate, q.v., with antimicrobial and antitumor activity. Prepn: E. F. Elslager, L. M. Werbel, GB 1345502 (1974 to Parke, Davis); E. F. Elslager et al., J. Med. Chem. 26, 1753 (1983); of water soluble salts: N. L. Colbry, EP 51415; idem, US 4376858 (1982, 1983 both to Warner-Lambert). In vitro antifolate activity and in vivo antitumor effect: J. R. Bertino et al., Biochem. Pharmacol. 28, 1983 (1979). Pharmacology: E. C. Weir et al., Cancer Res. 42, 1696 (1982); R. C. Jackson et al., Adv. Enzyme Regul. 22, 187 (1984). GC-MS determn in human plasma: P. L. Stetson, W. D. Ensminger, J. Chromatogr. 383, 69 (1986). Clinical evaluation with leucovorin vs Pneumocystis carinii in patients with AIDS: C. J. Allegra et al., N. Engl. J. Med. 317, 978 (1987). Review of pharmacology and clinical efficacy: J. T. Lin, J. R. Bertino, J. Clin. Oncol. 5, 2032-2040 (1987); P. J. O'Dwyer et al., NCI Monogr. 5, 105-109 (1987).

Nordihydroguaiaretic Acid CAS Registry Number: 27686-84-6 (meso-form); 500-38-9 (unspecified stereo)

CAS Name: (R*,S*)-4,4'-(2,3-Dimethyl-1,4-butanediyl)bis[1,2-benzenediol]
Additional Names: meso-4,4'-(2,3-dimethyltetramethylene)dipyrocatechol; 2,3-bis(3,4-dihydroxybenzyl)butane; b,g-dimethyl...
Literature References: Lipoxygenase inhibitor; occurs as the meso-form in the resinous exudate of the creosote bush, Larrea divaricata, Zygophyllaceae (Covillea tridentata). Isoln: C. W. Waller, O. Gisvold, J. Am. Pharm. Assoc. 34, 78 (1945). Prepn from guaiaretic acid dimethyl ether: G. Schroeter et al., Ber. 51, 1587 (1918); R. D. Haworth et al., J. Chem. Soc. 1934, 1423. Synthesis: S. V. Lieberman et al., J. Am. Chem. Soc. 69, 1540 (1947); and configuration of naturally occurring form: C. W. Perry et al., J. Org. Chem. 37, 4371 (1972). Use as antioxidant: W. M. Lauer, US 2373192 (1945 to U. S. Secr'y of Agriculture). Antiproliferative effect on cultured keratinocytes: D. I. Wilkinson, E. K. Orenberg, Int. J. Dermatol. 26, 660 (1987); on cultured glioma cells: D. E. Wilson et al., J. Neurosurg. 71, 551 (1989). Clinical trial in actinic keratoses: E. A. Olsen et al., J. Am. Acad. Dermatol. 24, 738 (1991).

Polyethylene Glycol CAS Registry Number: 25322-68-3 聚乙二醇

CAS Name: a-Hydro-w-hydroxypoly(oxy-1,2-ethanediyl)
Additional Names: macrogol; PEG
Trademarks: Carbowax (Union Carbide); Pluracol E (BASF); Poly-G (Olin); Polyglycol E (Dow)
Literature References: Liquid and solid polymers of the general formula H(OCH2CH2)nOH, where n is greater than or equal to 4. In general, each PEG is followed by a number which corresponds to its average mol wt. Synthesis: Fordyce, Hibbert, J. Am. Chem. Soc. 61, 1905, 1910 (1939). Polyethylene glycols are compds of low toxicity: Smyth et al., J. Am. Pharm. Assoc. Sci. Ed. 39, 349 (1950). Toxicity data (PEG 400): W. Bartsch et al., Arzneim.-Forsch. 26, 1581 (1976). Reviews: Glycols, G. O. Curme, F. Johnston, Eds. (Reinhold, New York, 1952) pp 176-202; Kastens in High Polymers, H. Mark et al., Eds., vol. 13 entitled Polyethers, part 1 (Interscience, New York, 1963) pp 169-189, 274-291; G. M. Powell, III in Handbook of Water-Soluble Gums Resins, R. L. Davidson, Ed. (McGraw-Hill, New York, 1980) pp 18/1-18/31. Book: Poly(Ethylene Glycol) Chemistry: Biotechnical and Biomedical Applications, J. M. Harris, Ed. (Plenum Press, New York, 1992) 385 pp. Series of articles on pegylation to enhance delivery of protein drugs: Adv. Drug Delivery Rev. 54, 453-609 (2002). Clinical evaluation as laxative: S. Chaussade, M. Minic, Aliment. Pharmacol. Ther. 17, 165 (2003).

Creosote, Wood CAS Registry Number: 8021-39-4 木材防腐油

Additional Names: Wood creosote; beechwood creosote
Trademarks: Creasote
Literature References: Liquid obtained from wood tars by distillation; composed chiefly of guaiacol and creosol, q.q.v. Analysis of constituents by GC-MS and HPLC: N. Ogata, T. Baba, Res. Commun. Chem. Pathol. Pharmacol. 66, 411 (1989). Acute toxicity: T. Miyazato et al., Oyo Yakuri 21, 899 (1981), C.A. 96, 28311h (1982). Chronic toxicity and carcinogenicity studies: eidem, ibid. 28, 909, 925 (1984), C.A. 102, 41238b, 57380c (1985). See also: Clinical Toxicology of Commercial Products, R. E. Gosselin et al., Eds. (Williams Wilkins, Baltimore, 5th ed., 1984) Section II, p 192. Review of toxicology and human exposure: Toxicological Profile for Wood Creosote, Coal Tar Creosote, Coal Tar, Coal Tar Pitch, and Coal Tar Pitch Volatiles (PB2003-100136, 2002) 394 pp.

Taribavirin CAS Registry Number: 119567-79-2 利巴韦林

CAS Name: 1-b-D-Ribofuranosyl-1H-1,2,4-triazole-3-carboximidamide
Additional Names: 1-b-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine; ribamidine
Percent Composition: C 39.51%, H 5.39%, N 2...
Literature References: Liver-targeting antiviral nucleoside analog; 3-carboxamidine prodrug of ribavirin, q.v. Prepn of hydrochloride: J. T. Witkowski et al., DE 2220246; eidem, US 3798209 (1972, 1974 both to ICN); idem et al., J. Med. Chem. 16, 935 (1973). Improved synthesis: G. D. Kini et al., ibid. 32, 1447 (1989); B. Gabrielsen et al., ibid. 35, 3231 (1992). In vitro and in vivo efficacy vs Phlebovirus: R. W. Sidwell et al., Antiviral Res. 10, 193 (1988); vs influenza: idem et al., ibid. 68, 10 (2005). LC/MS/MS determn in plasma: Y. Liu et al., J. Chromatogr. B 832, 17 (2006). Liver-targeting properties and safety profile in animals: C. Lin et al., Antivir. Chem. Chemother. 14, 145 (2003). Mechanism of action study: J. Z. Wu et al., Antimicrob. Agents Chemother. 48, 4006 (2004). Clinical pharmacokinetics in hepatitis C patients: S. Aora et al., J. Clin. Pharmacol. 45, 275 (2005).

Insulin Glargine CAS Registry Number: 160337-95-1 甘精胰岛素

CAS Name: 21A-Glycine-30Ba-L-arginine-30Bb-L-arginine-insulin (human)
Additional Names: [Gly(A21),Arg(B31),Arg(B32)]insulin (human)Trademarks: Lantus (Aventis)
Literature References: Long-acting analog of human insulin produced by recombinant DNA technology. Prepn: M. Dörschug, DE 3837825; idem, US 5656722 (1990, 1997 both to Hoechst). Characterization of receptor interaction: L. Berti et al., Horm. Metab. Res. 30, 123 (1998). Clinical pharmacodynamics: L. Heinemann et al., Diabetes Care 23, 644 (2000); pharmacokinetics: D. R. Owens et al., ibid. 813. Clinical trial in type 1 diabetics: R. E. Ratner et al., ibid. 639. Review of clinical experience: P. S. Gillies et al., Drugs 59, 253-260 (2000).

Lidocaine CAS Registry Number: 137-58-6 利多卡因

CAS Name: 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide
Additional Names: 2-diethylamino-2',6'-acetoxylidide; w-diethylamino-2,6-dimethylacetanilide; lignocaine
Trademarks: Cuivasil (IDC)...
Literature References: Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic. Prepn: N. M. Löfgren, B. J. Lundqvist, US 2441498 (1948 to Astra); A. D. H. Self, A. P. T. Easson, GB 706409 (1954 to May Baker); I. P. S. Hardie, E. S. Stern, GB 758224 (1956 to J. F. Macfarlane Co.); Zhuravlev, Nikolaev, Zh. Obshch. Khim. 30, 1155 (1960). Toxicity studies: E. R. Smith, B. R. Duce, J. Pharmacol. Exp. Ther. 179, 580 (1971); G. H. Kronberg et al., J. Med. Chem. 16, 739 (1973). Review of pharmacokinetics: N. L. Benowitz, W. Meister, Clin. Pharmacokinet. 3, 177 (1978). Review of action as local anesthetic: Löfgren, Studies on Local Anesthetics: Xylocaine, A New Synthetic Drug (Hoeggstroms, Stockholm, 1948); Cooper, Pharm. J. 171, 68 (1953). Reviews of anti-arrhythmic agents: J. L. Anderson et al., Drugs 15, 271 (1978); L. H. Opie, Lancet 1, 861 (1980); E. Carmeliet, Ann. N.Y. Acad. Sci. 427, 1 (1984). Comprehensive description: K. Groningsson et al., Anal. Profiles Drug Subs. 14, 207-243 (1985); M. F. Powell, ibid. 15, 761-779 (1986). Review of use in treatment of postherpetic neuralgia: P. S. Davies, B. S. Galer, Drugs 64, 937-947 (2004).