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

Fomepizole CAS Registry Number: 7554-65-6 4-甲基吡唑

CAS Name: 4-Methyl-1H-pyrazole
Additional Names: 4-MP
Trademarks: Antizol (Orphan Med.)
Percent Composition: C 58.52%, H 7.37%, N 34.12%
Literature References: Alcohol dehydrogenase inhibitor. Prepn: H. Pechmann, E. Burkard, Ber. 33, 3590 (1900); D. S. Noyce et al., J. Org. Chem. 20, 1681 (1955); T. Momose et al., Heterocycles 30, 789 (1990). Inhibition of human liver alcohol dehydrogenase: T.-K. Li, H. Theorell, Acta Chem. Scand. 23, 892 (1969). Toxicity study: G. Magnusson et al., Experientia 28, 1198 (1972). GC determn in plasma and urine: R. Achari, M. Mayersohn, J. Pharm. Sci. 73, 690 (1984). Clinical pharmacology: D. Jacobsen et al., Alcohol. Clin. Exp. Res. 12, 516 (1988). Pharmacokinetics: eidem, Eur. J. Clin. Pharmacol. 37, 599 (1989). Clinical trial in ethylene glycol poisoning: J. Brent et al., N. Engl. J. Med. 340, 832 (1999); in methanol poisoning: idem et al., ibid. 344, 424 (2001). Review: J. Likforman et al., J. Toxicol. Clin. Exp. 7, 373-382 (1987). Review of use in methanol poisoning: M. B. Mycyk, J. B. Leikin, Am. J. Therapeut. 10, 68-70 (2003).

Fidarestat CAS Registry Number: 136087-85-9; 105300-43-4 (unspecified) 非达司他

CAS Name: (2S,4S)-6-Fluoro-2,3-dihydro-2',5'-dioxospiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide
Additional Names: (2S,4S)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carbo...
Literature References: Aldose reductase inhibitor for treatment of diabetic complications. Prepn (stereo unspec): M. Kurono, et al., EP 193415; eidem, US 4740517 (1986, 1988 both to Sanwa). Prepn of isomers: T. Yamaguchi et al., Arzneim.-Forsch. 44, 344 (1994). Pharmacological profile: K. Mizuno et al. in Current Concepts of Aldose Reductase and Its Inhibitions, N. Sakamoto et al., Eds. (Elsevier, Amsterdam, 1990) pp 89-96. Configuration and crystal structure of complex with aldose reductase: M. Oka et al., J. Med. Chem. 43, 2479 (2000). Clinical efficacy in diabetic peripheral neuropathy: N. Hotta et al., Diabetes Care 24, 1776 (2001). Clinical suppression of sorbitol accumulation in erythrocytes of diabetic patients: T. Asano et al., J. Diabetes Complications 16, 133 (2002); eidem, ibid. 18, 336 (2004). Review of clinical development: N. Giannoukakis, Curr. Opin. Invest. Drugs 4, 1233-1239 (2003).

Zopolrestat CAS Registry Number: 110703-94-1 唑泊司他

CAS Name: 3,4-Dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid
Additional Names: 2-[4-oxo-3-[5-(trifluoromethyl)benzothiazol-2-ylmethyl]-3,4-dihydrophthal...
Literature References: Aldose reductase inhibitor. Prepn: B. L. Mylari et al., EP 222576; E. R. Larson, B. L. Mylari, US 4939140 (1987, 1990 both to Pfizer); B. L. Mylari et al. J. Med. Chem. 34, 108 (1991). Pharmacology: B. Tesfamariam et al., J. Cardiovasc. Pharmacol. 21, 205 (1993); B. Tesfamariam et al., Am. J. Physiol. 265, H1189 (1993). Clinical pharmacokinetics: P. B. Inskeep et al., J. Clin. Pharmacol. 34, 760 (1994).

Zenarestat CAS Registry Number: 112733-06-9 折那司他

CAS Name: 3-[(4-Bromo-2-fluorophenyl)methyl]-7-chloro-3,4-dihydro-2,4-dioxo-1(2H)-quinazolineacetic acid
Additional Names: 3-(4-bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1,2,3,4-tetrahydroquinaz...
Literature References: Aldose reductase inhibitor. Prepn: M. Hashimoto et al., EP 218999; eidem, US 4734419 (1987, 1988 both to Fujisawa). Inhibition kinetics and effect on sorbitol accumulation: S. Ao et al., Metabolism 40, 77 (1991). Pharmacokinetics and metabolism in diabetic rats: Y. Tanaka et al., Drug Metab. Dispos. 21, 677 (1993). Clinical pharmacology: M. Kanamaru et al., J. Clin. Pharmacol. 33, 1122 (1993).

Epalrestat CAS Registry Number: 82159-09-9 依帕司他

CAS Name: (5Z)-5-[(2E)-2-Methyl-3-phenyl-2-propenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid
Additional Names: 5-[(E,E)-b-methylcinnamylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid; 3-...
Literature References: Aldose reductase inhibitor. Prepn: T. Tadao et al., EP 47109; eidem, US 4464382 (1982, 1984 both to Ono Pharmaceutical). Inhibitory effect on aldose reductase in vitro: H. Terashima et al., J. Pharmacol. Exp. Ther. 229, 226 (1983). Effect on motor nerve conduction and sorbitol levels in diabetic rats: R. Kikkawa et al., Diabetologia 24, 290 (1983). Effect in rats on peripheral nerve dysfunction: eidem, Metabolism 33, 212 (1984); on retinal microangiopathy: K. Kojima et al., Jpn. J. Ophthalmol. 29, 99 (1985).

Adrenolutin CAS Registry Number: 642-75-1 肾上腺黄素

CAS Name: 1-Methyl-1H-indole-3,5,6-triol
Additional Names: N-methyl-5,6-dihydroxyindoxyl; 3,5,6-trihydroxy-N-methylindole
Percent Composition: C 60.33%, H 5.06%, N 7.82%, O 26.79%
Literature References: Alkaline rearrangement product of adrenochrome. Isoln and identification: Lund, Acta Pharmacol. Toxicol. 5, 75 (1949). Structure and synthesis: Balsinger et al., Helv. Chim. Acta 36, 708 (1953); Heacock, Mahon, Can. J. Chem. 36, 1550 (1958). NMR studies and its existence in the ketonic form in solution: Powell, Heacock, Chim. Ther. 7, 133 (1972).

Tetrahydropapaveroline CAS Registry Number: 4747-99-3 四氢维洛林

CAS Name: 1-[(3,4-Dihydroxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-isoquinolinediol
Additional Names: 1-(3,4-dihydroxybenzyl)-1,2,3,4-tetrahydro-6,7-isoquinolinediol; 6,7-dihydroxy-1-(3,4-dihydro...
Literature References: Alkaloid deriv of dopamine and a biosynthetic precursor of morphine, q.v. Prepn of the racemic hydrochloride: F. L. Pyman, J. Chem. Soc. 95, 1610 (1909); of the (+)- and (-)-form hydrochlorides: S. Teitel et al., J. Med. Chem. 15, 845 (1972). Chromatographic study: K. D. McMurtrey et al., J. Liq. Chromatogr. 3, 663 (1980). Possible role of THP in the biochemical mediation of alcohol addiction: V. E. Davis, M. J. Walsh, Science 167, 1005 (1970); G. Cohen, M. Collins, ibid. 1749; R. D. Meyers, C. L. Melchior, ibid. 196, 554 (1977); M. Sandler et al., Prog. Clin. Biol. Res. 90, 215 (1982). Biosynthetic study: D. K. Choudhary, B. L. Kaul, Indian Drugs 19, 229 (1982). In vivo and in vitro effects on rat pituitary function: D. R. Britton et al., Biochem. Pharmacol. 31, 1205 (1982). Effect on dopaminergic neurons: I. S. Hoffman, L. X. Cubeddu, J. Pharmacol. Exp. Ther. 220, 16 (1982). Comparison to opioid effects in brain regions: G. R. Siggins et al., Prog. Clin. Biol. Res. 90, 275 (1982).

Muscarine CAS Registry Number: 300-54-9 [(2S,4R,5S)-4-羟基-5-甲基四氢呋喃-2-基]甲基-三甲基铵

CAS Name: [2S-(2a,4b,5a)]-Tetrahydro-4-hydroxy-N,N,N,5-tetramethyl-2-furanmethanaminium
Literature References: Alkaloid from the red variety of Amanita muscaria (L.) Pers., Agaricaceae, the fly fungus, a poisonous mushroom. Also found in some other fungi: Inocybe patouillardi; I. fastigiata, I. umbrina; I. rimosa. Isoln procedure for the naturally occurring L-(+)-form: Kuehl et al., J. Am. Chem. Soc. 77, 6663 (1955); Eugster, Helv. Chim. Acta 39, 1002 (1956). Structure and synthesis of racemate: Kögl et al., Rec. Trav. Chim. 76, 109 (1957); Kögl et al., Experientia 13, 137, 138 (1957); Cox et al., Helv. Chim. Acta 41, 229 (1958). Alternate syntheses: GB 828395 (1960 to Hoffmann-La Roche); Matsumoto et al., Tetrahedron 25, 5889 (1969); W. C. Still, J. A. Schneider, J. Org. Chem. 45, 3375 (1980). Synthesis of muscarine: Whiting et al., Can. J. Chem. 50, 3322 (1972); A. M. Mubarak, D. M. Brown, Tetrahedron Lett. 21, 2453 (1980); eidem, J. Chem. Soc. Perkin Trans. 1 1982, 809; S. Pochet, T. Huynhdinh, J. Org. Chem. 47, 193 (1982). Chemistry and pharmacology: Waser, Pharmacol. Rev. 13, 465-515 (1961). Toxicity study: P. J. Fraser, Br. J. Pharmacol. 12, 47 (1957). Reviews: C. H. Eugster, Adv. Org. Chem. 2, 427-455 (1960); S. Wilkinson, Q. Rev. Chem. Soc. 15, 153-171 (1961). Configurational relationship in the muscarine series: Bollinger, Eugster, Helv. Chim. Acta 54, 2704 (1971).

Hasubanonine CAS Registry Number: 1805-85-2 蓬花宁碱

CAS Name: 7,8-Didehydro-3,4,7,8-tetramethoxy-17-methylhasubanan-6-one
Percent Composition: C 67.54%, H 7.29%, N 3.75%, O 21.42%
Literature References: Alkaloid having a modified morphinan skeleton with a five membered heterocyclic ring, hitherto unknown in natural sources. (Alkaloids with this unique skeleton are called hasubanan alkaloids; see S. Shiotani, T. Kometani, Tetrahedron Lett. 1976, 767 for synthesis of hasubanan skeleton). Isolated from Stephania japonica Miers, Menispermaceae: Kondo et al., Annu. Rep. Itsuu Lab. 2, 35 (1951); Satomi, ibid. 3, 37 (1953); Kondo, Satomi, ibid. 8, 41 (1957); C.A. 47, 5951f (1953); 48, 2728c (1954); 51, 17956i (1957). Structure: Tomita et al., Tetrahedron Lett. 1964, 2937; eidem, Chem. Pharm. Bull. 13, 538 (1965). Total synthesis: Ibuka et al., Tetrahedron Lett. 1970, 4811; Chem. Pharm. Bull. 22, 782 (1974). Biosynthesis: A. R. Battersby et al., Chem. Commun. 1974, 773; eidem, J. Chem. Soc. Perkin Trans. 1 1981, 2010, 2016, 2030. Review: Y. Inubushi, T. Ibuka in The Alkaloids vol. XVI, R. H. F. Manske, Ed. (Academic Press, New York, 1977) pp 393-428.

Corydaline CAS Registry Number: 518-69-4 延胡索甲素

CAS Name: (13S-trans)-5,8,13,13a-Tetrahydro-2,3,9,10-tetramethoxy-13-methyl-6H-dibenzo[a,g]quinolizine
Additional Names: 2,3,9,10-tetramethoxy-13a-methyl-13ab-berbine; d-corydaline
Percent C...
Literature References: Alkaloid isolated from many species of Corydalis. Discovery in C. tuberosa: Wackenroder, Kustner's Arch. 8, 423 (1826), as cited in: C. Wehmer, Die Pflanzenstoffe I (G. Fischer, Jena, 1929) p 389. Isoln from Corydalis aurea Willd. and C. solida (L.) Swartz, Fumariaceae: Manske, Can. J. Res. 16B, 81 (1938); Can. J. Chem. 34, 1 (1956). Structure: von Bruchhausen, Stippler, Arch. Pharm. 265, 152 (1927). Synthesis: Späth, Kruta, Ber. 62, 1024 (1929); T. Kametani et al., J. Chem. Soc. Perkin Trans. 1 1977, 1151; M. Cushman, F. W. Dekon, Tetrahedron 1978, 1435; Z. Kiparissides et al., Can. J. Chem. 58, 2770 (1980). Stereochemistry: Bersch, Arch. Pharm. 291, 595 (1958); Jeffs, Experientia 21, 690 (1965). Pharmacology: Berezhinskaya, C.A. 78, 119087j (1973). Toxicity study: R. C. Anderson, K. K. Chen, Fed. Proc. 5, 163 (1946).