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

Maclurin CAS Registry Number: 519-34-6 桑橙素,2,3',4,4',6-五羟基二苯甲酮

CAS Name: (3,4-Dihydroxyphenyl)(2,4,6-trihydroxyphenyl)methanone
Additional Names: 2,3',4,4',6-pentahydroxybenzophenone; morintannic acid; moritannic acid; laguncurin; kino-yellow; C.I. Natural...
Literature References: From wood of Chlorophora tinctoria (L.) Gaud. (Morus tinctoria L., Maclura tinctoria (L.) D. Don), Moraceae (old fustic): Haley, Bassin, J. Am. Pharm. Assoc. 40, 111 (1951); Laidlow, Smith, Chem. Ind. (London) 1959, 1604; from Morus alba Linn., Moraceae: Spada et al., Gazz. Chim. Ital. 86, 46 (1956). Identity with laguncurin and kino-yellow: Nierenstein, Q. J. Pharm. Pharmacol. 16, 11 (1943). See also Colour Index vol. 4 (3rd ed., 1971) p 4627.

Flindersine CAS Registry Number: 523-64-8 2,2-二甲基-2,6-二氢-吡喃并[3,2-c]喹啉-5-酮

CAS Name: 2,6-Dihydro-2,2-dimethyl-5H-pyrano[3,2-c]quinolin-5-one
Additional Names: 2,2'-dimethyl-a-pyrano(5',6',3,4)-2(1H)-quinolone
Percent Composition: C 73.99%, H 5.77%, N 6.16%, O 14.08...
Literature References: From wood of Flindersia australis R. Br., Rutaceae: Matthes, Schreiber, Ber. Dtsch. Pharm. Ges. 24, 385 (1914). Structure: Brown et al., Aust. J. Chem. 7, 348 (1954). Synthesis: eidem, ibid. 9, 277 (1956); Piozzi et al., Gazz. Chim. Ital. 99, 711 (1969); Bowman et al., Chem. Commun. 1970, 666; Huffman, Hsu, Tetrahedron Lett. 1972, 141.

Fustin CAS Registry Number: 20725-03-5 黄颜木素

CAS Name: (2R,3R)-rel-2-(3,4-Dihydroxyphenyl)-2,3-dihydro-3,7-dihydroxy-4H-1-benzopyran-4-one
Additional Names: 3,3',4',7-tetrahydroxyflavanone; dihydrofisetin
Percent Composition: C 62.50%,...
Literature References: From wood of Rhus cotinus L. (Venice sumac) and R. succedanea L., Anacardiaceae: Schmid, Ber. 19, 1734 (1886); from Gleditsia triacanthos L., Leguminosae: Chadenson et al., Compt. Rend. 249, 1362 (1955). Structure: Oyamada, Ann. 538, 44 (1939). Stereochemistry: Weinges, Ann. 627, 229 (1959); Roux, Paulus, Biochem. J. 77, 315 (1960); Gaffield, Tetrahedron 26, 4093 (1970).

Thujopsene CAS Registry Number: 470-40-6 罗汉柏烯

CAS Name: 1,1a,4,4a,5,6,7,8-Octahydro-2,4a,8,8-tetramethylcyclopropa[d]naphthalene
Additional Names: widdrene
Percent Composition: C 88.16%, H 11.84%
Literature References: From wood oil of the Japanese Hiba tree, Thujopsis dolobrata Sieb, and Zucc., Cupressaceae: Yano, J. Soc. Chem. Ind. Jpn. 16, 443 (1913); Uchida, ibid. 31, 501 (1928). Identity with widdrene: Erdtman, Thomas, Acta Chem. Scand. 12, 267 (1958). Structure: Norin, ibid. 15, 1676 (1961). Stereochemistry: Sisido et al., J. Org. Chem. 26, 1964 (1961); Norin Acta Chem. Scand. 17, 738 (1963). Synthesis: Dauben, Ashcraft, J. Am. Chem. Soc. 85, 3673 (1963); Büchi, White, ibid. 86, 2884 (1964).

Ylangene CAS Registry Number: 14912-44-8 [1S,2R,6R,7R,8S,(+)]-1,3-二甲基-8-(1-甲基乙基)三环[4.4.0.0(2,7)]癸-3-烯

CAS Name: 1,3-Dimethyl-8-(1-methylethyl)tricyclo[4.4.0.02,7]dec-3-ene
Additional Names: (1S,2R,6R,7R,8S)-(+)-8-isopropyl-1,3-dimethyltricyclo[4.4.0.02,7]dec-3-ene; a-ylangene
Percent Composi...
Literature References: From ylang-ylang oil: Heraut, Dimitrov, Chem. Listy 46, 432 (1952); from oil of birch buds: Holub et al., Collect. Czech. Chem. Commun. 24, 3730 (1959); from oil of Juniperus oxycedrus Linn., Cupressaceae: Motl et al., ibid. 25, 1656 (1960). Structure: Motl et al., Chem. Ind. (London) 1963, 1759; Hunter, Brogden, J. Org. Chem. 29, 982 (1964); Motl et al., Tetrahedron Lett. 1965, 451. Stereoisomer of copaene, q.v. Total synthesis of (±)-form: Heathcock et al., J. Am. Chem. Soc. 89, 4133 (1967); Corey, Watt, ibid. 95, 2303 (1973).

Lacosamide CAS Registry Number: 175481-36-4 拉科酰胺

CAS Name: (2R)-2-(Acetylamino)-3-methoxy-N-(phenylmethyl)propanamide
Additional Names: (R)-N-benzyl-2-acetamido-3-methoxypropionamide; erlosamide; harkoseridePercent Composition: C 62.38%, H 7....
Literature References: Functionalized amino acid with demonstrated anticonvulsant and analgesic activity. Prepn: D. Choi et al., J. Med. Chem. 39, 1907 (1996); H. Kohn, WO 9733861; idem, US 5773475 (1997, 1998 both to Research Corp. Technol.). Improved prepn and anticonvulsant activity: S. V. Andurkar et al., Tetrahedron: Asymmetry 9, 3841 (1998). Mode of action study: G. Lees et al., Neuropharmacology 50, 98 (2006). Evaluation in animal models of seizure: G. E. Duncan, H. Kohn, Epilepsy Res. 67, 81 (2005); of inflammatory pain: T. Stöhr et al., Eur. J. Pain 10, 241 (2006). Clinical evaluation in neuropathic pain: G. McCleane et al., Neurosci. Lett. 352, 117 (2003). Review of clinical development: C. A. Hovinga, IDrugs 6, 479-485 (2003).

Mevastatin CAS Registry Number: 73573-88-3 美伐他汀

CAS Name: (2S)-2-Methylbutanoic acid (1S,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-7-methyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester
Additional Names: 7-[1,2,6...
Literature References: Fungal metabolite which is a potent inhibitor of HMG-CoA reductase, the rate controlling enzyme in cholesterol biosynthesis. Isoln from Penicillium citrinum: A. Endo et al., DE 2524355 corresp to US 3983140 (1975, 1976 to Sankyo). Isoln from P. brevicompactum, crystal and molecular structure: A. G. Brown et al., J. Chem. Soc. Perkin Trans. 1 1976, 1165. Inhibition of HMG-CoA reductase activity: A. Endo et al., FEBS Lett. 72, 323 (1976); M. S. Brown et al., J. Biol. Chem. 253, 1121 (1978). Therapeutic effects in primary hypercholesterolemia: A. Yamamoto et al., Atherosclerosis 35, 259 (1980). Total synthesis: N. Y. Wang et al., J. Am. Chem. Soc. 103, 6538 (1981); M. Hirama, M. Uei, ibid. 104, 4251 (1982); N. N. Girotra, N. L. Wendler, Tetrahedron Lett. 23, 5501 (1982); C.-T. Hsu et al., J. Am. Chem. Soc. 105, 593 (1983); P. A. Grieco et al., ibid. 1403; D. L. J. Clive et al., J. Am. Chem. Soc. 110, 6914 (1988). Review of syntheses: T. Rosen, C. H. Heathcock, Tetrahedron 42, 4909-4951 (1986). Review of mevastatin and related compounds: A. Endo, J. Med. Chem. 28, 401-405 (1985).

Lovastatin CAS Registry Number: 75330-75-5 洛伐他汀

CAS Name: (2S)-2-Methylbutanoic acid (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester
Additional Names: (...
Literature References: Fungal metabolite; potent inhibitor of HMG-CoA reductase, the rate controlling enzyme in cholesterol biosynthesis. Isoln from Monascus ruber: A. Endo, J. Antibiot. 32, 852 (1979); from Aspergillus terreus: R. L. Monaghan et al., US 4231938 (1980 to Merck Co.). Structure and biochemical properties: A. W. Alberts et al., Proc. Natl. Acad. Sci. USA 77, 3957 (1980). Total synthesis: M. Hirama, M. Iwashita, Tetrahedron Lett. 24, 1811 (1983). Review of syntheses: T. Rosen, C. H. Heathcock, Tetrahedron 42, 4909-4951 (1986). Biosynthesis: M. D. Greenspan, J. B. Yudkovitz, J. Bacteriol. 162, 704 (1985); R. N. Moore et al., J. Am. Chem. Soc. 107, 3694 (1985). HPLC determn in plasma and bile: R. J. Stubbs et al., J. Chromatogr. 383, 438 (1986). Clinical pharmacology: S. M. Grundy, G. L. Vega, J. Lipid Res. 26, 1464 (1985). Clinical comparison with gemfibrozil, q.v.: M. J. Tikkanen et al., Am. J. Cardiol. 62, 35J (1988). Review of clinical experience: J. A. Tobert, Am. J. Cardiol. 62, 28J-34J (1988). Comprehensive description: G. S. Brenner et al., Anal. Profiles Drug Subs. Excip. 21, 277-305 (1992). Prevention of acute coronary events in men and women with average cholesterol levels: J. R. Downs et al., J. Am. Med. Assoc. 279, 1615 (1998).

Oosporein CAS Registry Number: 475-54-7 卵孢霉素

CAS Name: 2,2',5,5'-Tetrahydroxy-4,4'-dimethyl[bi-1,4-cyclohexadien-1-yl]-3,3',6,6'-tetrone
Additional Names: 3,3',6,6'-tetrahydroxy-5,5'-dimethyl-2,2'-bi-p-benzoquinone; chaetomidin; iso-oospo...
Literature References: Fungal pigment isolated from Oospora colorans van Beyma.: Kögl, van Wessem, Rec. Trav. Chim. 63, 5 (1944); from Chaetonium aureum Chivers and identity with chaetomidin: Lloyd et al., J. Chem. Soc. 1955, 2163; from Acremonium spp: Divekar et al., Can. J. Chem. 37, 2097 (1959); from Beauveria bassiana (Bals.) Vuill.: Vining et al., Can. J. Microbiol. 8, 931 (1962). Identity with iso-oosporein: Smith, Thomson, Tetrahedron 10, 148 (1960). Synthesis: J. Kalamar et al., Helv. Chim. Acta 57, 2368 (1974). Biosynthesis: E. Steiner et al., ibid. 2377.

Phenicin CAS Registry Number: 128-68-7 (3Z)-3-(2,3-二羟基-4-甲基-6-氧代-1-环己-2,4-二烯亚基)-6-甲基环己-5-烯-1,2,4-三酮

CAS Name: 2,2'-Dihydroxy-4,4'-dimethyl[bi-1,4-cyclohexadien-1-yl]-3,3',6,6'-tetrone
Additional Names: 3,3'-dihydroxy-5,5'-dimethyl-2,2'-bi-p-benzoquinone; phoenicin
Percent Composition: C 61...
Literature References: Fungal pigment produced by Penicillium phoeniceum and P. rubrum: Friedheim, Helv. Chim. Acta 21, 1464 (1938); Charollais et al., Arch. Sci. 16, 474 (1963). Synthesis: Posternak et al., Helv. Chim. Acta 26, 2031 (1943); Musso, Beecken, Ber. 92, 1416 (1959); J. Kalamar et al., Helv. Chim. Acta 57, 2368 (1974). Biosynthesis: E. Steiner et al., ibid. 2377.