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

Tenuazonic Acid CAS Registry Number: 610-88-8 细交链孢菌酮酸

CAS Name: (5S)-3-Acetyl-1,5-dihydro-4-hydroxy-5-[(1S)-1-methylpropyl]-2H-pyrrol-2-one
Additional Names: L-3-acetyl-5-sec-butyl-4-hydroxy-3-pyrrolin-2-one; L-3-acetyl-5-sec-butyltetramic acid Literature References: Mycotoxin produced by Alternaria alternata and other fungal species; contaminant found in wheat and other grains, sunflower seeds, tomatoes and other fruits. Isoln from culture filtrates of Alternaria tenuis Auct.: T. Rosett et al., Biochem. J. 67, 390 (1957). Structure: C. E. Stickings, Biochem. J. 72, 332 (1959). Biosynthesis: C. E. Stickings, R. J. Townsend, ibid. 78, 412 (1961). Chemical synthesis: R. N. Lacey, J. Chem. Soc. 1954, 850; S. A. Harris et al., J. Med. Chem. 8, 478 (1965); R. Schobert et al., Org. Biomol. Chem. 2, 3524 (2004). Tumor inhibitory properties: E. A. Kaczka et al., Biochem. Biophys. Res. Commun. 14, 54 (1964); C. O. Gitterman et al., Cancer Res. 24, 440 (1964). Toxicity of isolates from agricultural samples: R. A. Meronuck et al., Appl. Microbiol. 23, 613 (1972). Review of analytical methods and occurrence in foods: P. M. Scott, J. AOAC Int. 84, 1809-1817 (2001).

Trichothecin CAS Registry Number: 6379-69-7 三线镰刀霉素

CAS Name: [4b(Z)]-12,13-Epoxy-4-[(1-oxo-2-butenyl)oxy]trichothec-9-en-8-one
Additional Names: 12,13-epoxy-4-hydroxytrichothec-9-en-8-one crotonate
Percent Composition: C 68.66%, H 7.28%, O 2...
Literature References: Mycotoxin with antibiotic activity. Produced by Trichothecium roseum: Freeman, Morrison, Nature 162, 30 (1948). Activity: G. G. Freeman, J. Gen. Microbiol. 12, 213 (1955). Structure: Godtfredsen, Vangedal, Proc. Chem. Soc. London 1964, 188; Gutzwiller et al., Helv. Chim. Acta 47, 2234 (1964). Biogenesis: Jones, Lowe, J. Chem. Soc. 1960, 3959. Biosynthetic studies: Achilladelis et al., J. Chem. Soc. Perkin Trans. 1 1972, 1425; Machida, Nozoe, Tetrahedron Lett. 1972, 1969; eidem, Tetrahedron 28, 5113 (1972).

Rhodinol CAS Registry Number: 6812-78-8 (S)-3,7-二甲基-7-辛烯-1-醇

CAS Name: (3S)-3,7-Dimethyl-7-octen-1-ol
Additional Names: a-citronellol
Percent Composition: C 76.86%, H 12.90%, O 10.24%
Literature References: Name that has been used to describe a group of related chemicals as well as a single chemical. The term, at times, was applied to what was considered the most important alcohol in geranium oil, 1-citronellol. See: Barbier, Bouveault, Ber. 29, 289 (1896). Prepn in pure form: Sutherland, J. Am. Chem. Soc. 73, 2385 (1951). Synthesis from cis-pinane: Rienäcker, Chimia 27, 97 (1973).

Quinine Iodosulfate CAS Registry Number: 7631-46-1 金鸡南-9-醇,6'-甲氧基-,(8α,9R)-,(三碘化氢)硫酸盐(盐)(4:2:3)

Additional Names: Herapathite; iodoquinine sulfate
Percent Composition: C 40.79%, H 4.45%, I 32.33%, N 4.76%, O 13.59%, S 4.08%
Literature References: Named after its discoverer, Herapath, an English physician.

Cyprenorphine CAS Registry Number: 4406-22-8 环丙诺啡

CAS Name: (5a,7a)-17-(Cyclopropylmethyl)-4,5-epoxy-3-hydroxy-6-methoxy-a,a-dimethyl-6,14-ethenomorphinan-7-methanol
Additional Names: N-(cyclopropylmethyl)-7,8-dihydro-7a-(1-hydroxy-1-methyleth...
Literature References: Narcotic antagonist closely related to diprenorphine, q.v. Prepn (7a- or 7b-linkage unspecified): BE 629070 (1963 to J. F. Macfarlan), C.A. 61, 13364g (1964); K. W. Bentley, US 3474101 (1969 to Reckitt Sons); of 7a: K. W. Bentley, D. G. Hardy, J. Am. Chem. Soc. 89, 3281 (1967). Activity in rats: K. W. Bentley et al., Nature 206, 102 (1965). Use in large animals: M. R. Jainudeen, Vet. Rec. 89, 686 (1971); K. R. Presnell et al., J. Wildl. Dis. 9, 336 (1973). Binding to neuroleptic receptors: A. Czlonkowski et al., Life Sci. 22, 953 (1978). Determn by HPLC: I. Jane, A. McKinnon, J. Chromatogr. 323, 191 (1985).

Sapropterin CAS Registry Number: 62989-33-7 沙丙蝶呤

CAS Name: (6R)-2-Amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-4(1H)-pteridinone
Additional Names: (6R)-L-erythro-tetrahydrobiopterin; dapropterin; R-THBP; 6R-BH4
Percent Composit...
Literature References: Natural cofactor of the aromatic amino acid hydroxylases required for catecholamine and serotonin biosynthesis. Identification of cofactor activity: S. Kaufman, Proc. Natl. Acad. Sci. USA 50, 1085 (1963). Prepn of (6R,S)-BH4: B. Schircks et al., Helv. Chim. Acta 61, 2731 (1978). Chromatographic separation of diastereoisomers: S. W. Bailey, J. E. Ayling, J. Biol. Chem. 253, 1598 (1978). Absolute configuration of natural isomer: W. L. F. Armarego et al., Aust. J. Chem. 35, 785 (1982). Stereospecific synthesis: S. Matsuura et al., Heterocycles 23, 3115 (1985); H. Sakai, T. Kanai, EP 191335; eidem, US 4713454 (1986, 1987 both to Shiratori; Suntory). Bioavailability: G. Kapatos, S. Kaufman, Science 212, 955 (1981). Effect on neurotransmitter monoamine biosynthesis: S. Miwa et al., Arch. Biochem. Biophys. 239, 234 (1985). LC determn in biological samples: Y. Tani, T. Ishihara, Life Sci. 46, 373 (1990). Therapeutic potential in hyperphenylalaninemia: S. Kaufman, J. Nutr. Sci. Vitaminol, Suppl., 601 (1992).

Methyleugenol CAS Registry Number: 93-15-2 甲基丁香酚, 甲基丁子香酚

CAS Name: 1,2-Dimethoxy-4-(2-propenyl)benzene
Additional Names: 4-allyl-1,2-dimethyoxybenzene; 4-allylveratrole; 3,4-dimethoxyallylbenzene; eugenol methyl ether
Percent Composition: C 74.13%...
Literature References: Natural constituent of the volatile oils of various plants, including cinnamon, clove, nutmeg, basil, and anise. Prepn: K. U. Matsmoto, Ber. 11, 122 (1878). Isoln from the bark of Cinnamomum oliveri: G. W. Hargreaves, J. Chem. Soc. 109, 751 (1916). Raman spectroscopy: B. Susz et al., Helv. Chim. Acta 19, 548 (1936). Toxicity: P. M. Jenner et al., Food Cosmet. Toxicol. 2, 327 (1964). HPLC determn in plasma: S. W. Graves, S. Runyon, J. Chromatogr. B 663, 255 (1995). GC/MS determn in basil cultivars: M. Miele et al., J. Agric. Food Chem. 49, 517 (2001). Biosynthesis in sweet basil: E. Lewinsohn et al., Plant Sci. 160, 27 (2000). Safety assessment: R. L. Smith et al., Food Chem. Toxicol. 40, 851 (2002).

Ergocristine CAS Registry Number: 511-08-0 麦角日亭宁麦角生物碱

CAS Name: (5'a)-12'-Hydroxy-2'-(1-methylethyl)-5'-(phenylmethyl)ergotaman-3',6',18-trione
Percent Composition: C 68.95%, H 6.45%, N 11.49%, O 13.12%
Literature References: Natural ergot alkaloid derived from lysergic acid; a member of the ergotoxine group. Isoln from ergot: Stoll, Burckhardt, Z. Physiol. Chem. 250, 1 (1937); Stoll, Hofmann, Helv. Chim. Acta 26, 1570 (1943). Structure: Stoll et al., ibid. 34, 1544 (1951). Separation and purification: Stoll, Hofmann, US 2447214 (1948 to Sandoz). Synthesis: Stadler et al., Helv. Chim. Acta 52, 1549 (1969).

Ergocornine CAS Registry Number: 564-36-3 麦角考宁

CAS Name: (5'a)-12'-Hydroxy-2',5'-bis(1-methylethyl)ergotaman-3',6',18-trione
Percent Composition: C 66.29%, H 7.00%, N 12.47%, O 14.24%
Literature References: Natural ergot alkaloid derived from lysergic acid; component of ergotoxine, q.v. Isoln from ergot: Stoll, Hofmann, Helv. Chim. Acta 26, 1570 (1943). Structure: Stoll et al., ibid. 34, 1544 (1951). Separation and purification: Stoll, Hofmann, US 2447214 (1948 to Sandoz). Synthesis: Stadler et al., Helv. Chim. Acta 52, 1549 (1969). Determn in ergot by capillary electrophoresis: K. Frach, G. Blaschke, J. Chromatogr. A 808, 247 (1998).

Apoptolidin CAS Registry Number: 194874-06-1 (8E,10E,12R,13R,14E,16E,18E)-12-羟基-13-甲基-20-氧代氧杂环二十-8,10,14,16,18-五烯-2,4,5-三基

CAS Name: O-2,6-Dideoxy-3-O-methyl-b-D-arabino-hexopyranosyl-(1®4)-2,6-dideoxy-3-C-methyl-a-L-arabino-hexopyranosyl-(1®8)-3,5,7-trideoxy-1-C-[(2S,4S,5S,8E,10E,12R,13R,14E,16E,18E)-12-[(6-deoxy-4-O...
Literature References: Natural product isolated from Nocardiopsis sp.; specifically induces apoptosis in transformed tumor cells. Isoln, properties and bioactivity: J. W. Kim et al., J. Antibiot. 50, 628 (1997). Structure: Y. Hayakawa et al., J. Am. Chem. Soc. 120, 3524 (1998). Partial synthesis: J. Schuppan et al., Tetrahedron Lett. 41, 621 (2000); K. C. Nicolaou et al., Chem. Commun. 2000, 307. Review of synthetic methods: P. T. Daniel et al., Angew. Chem. Int. Ed. 45, 872-893 (2006).