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

Bethanidine CAS Registry Number: 55-73-2 倍他尼定

CAS Name: N,N'-Dimethyl-N''-(phenylmethyl)guanidine
Additional Names: 1-benzyl-2,3-dimethylguanidine; N-benzyl-N',N''-dimethylguanidine
Percent Composition: C 67.76%, H 8.53%, N 23.71%
Literature References: Adrenergic neuron blocking agent. Prepn: Walton, Ruffell, US 3168562 (1965 to Wellcome Found.); GB 1084461 and GB 1111564 (1967 and 1968 to Wellcome Found.). Pharmacology: A. L. A. Boura, A. F. Green, Br. J. Pharmacol. 20, 36 (1963); J. A. Oates et al., Ann. N.Y. Acad. Sci. 179, 302 (1971). Pharmacokinetics: C. N. Corder, J. Clin. Pharmacol. 19, 428 (1979). HPLC determn in plasma: J. R. Shipe et al., Clin. Chem. 29, 1793 (1983). Anti-arrhythmic activity: M. B. Bacaner, D. G. Benditt, Am. J. Cardiol. 50, 728 (1982); J. C. Somberg et al., ibid. 54, 343 (1984). Review: A. F. Green, Br. J. Clin. Pharmacol. 13, 25-34 (1982).

Uscharidin CAS Registry Number: 24321-47-9 (2S,3R)-14-羟基-19-氧代-2,3-[[(2S,3R,6R)-四氢-3-羟基-6-甲基-4-氧代-2H-吡喃-3,2-二基]二氧基]心甾-20(22)-烯内酯

CAS Name: [2a(2S,3R,6R),3b,5a]-14-Hydroxy-19-oxo-2,3-[(tetrahydro-3-hydroxy-6-methyl-4-oxo-2H-pyran-3,2-diyl)bis(oxy)]card-20(22)-enolide
Percent Composition: C 65.64%, H 7.22%, O 27.14%
Literature References: African arrow poison and cardiac glycoside produced by Calotropis procera R. Br., Asclepiadaceae: Hesse et al., Ann. 566, 130 (1950). Prepn by hydrolysis of uscharin with 2N H2SO4 in methanol: Hesse et al., Ann. 537, 67 (1938); by treatment of voruscharin with mercuric chloride: Hesse, Ludwig, Ann. 632, 158 (1960). Structure: Crout et al., J. Chem. Soc. 1964, 2187. Revised structure: Brüschweiler et al., Helv. Chim. Acta 52, 2276 (1969). Stereochemistry: H. T. A. Cheung, T. R. Watson, J. Chem. Soc. Perkin Trans. 1 1980, 2162.

Calotropin CAS Registry Number: 1986-70-5 牛角瓜甙

CAS Name: [2a(2S,3S,4S,6R),3b,5a]-14-Hydroxy-19-oxo-3,2-[(tetrahydro-3,4-dihydroxy-6-methyl-2H-pyran-2,3-diyl)bis(oxy)]card-20(22)-enolide
Percent Composition: C 65.40%, H 7.57%, O 27.04%
Literature References: African arrow poison isolated from milk sap of Calotropis procera Dryand., Asclepiadaceae. Isolation: Lewin, Arch. Exp. Pathol. Pharmakol. 71, 142 (1913); Hesse et al., Ann. 526, 252 (1936); 566, 130 (1950); Rajagopalan et al., Helv. Chim. Acta 38, 1809 (1955). Isoln from Asclepias curassavica L., Asclepiadaceae: S. M. Kupchan et al., Science 146, 1685 (1964). Structure: G. Hesse, G. Lettenbauer, Ann. 623, 142 (1959); Hesse et al., ibid. 625, 157, 161 (1959); D. G. H. Crout et al., Tetrahedron Lett. 1963, 63; J. Chem. Soc. 1964, 2187. Extraction from C. procera R.Br. and toxicity: F. Brüschweiler et al., Helv. Chim. Acta 52, 2086 (1969). Revised structure: eidem, ibid. 2276. Sequestration by larvae of Monarch butterfly Danaus plexippus L.: J. N. Sieber et al., J. Chem. Ecol. 6, 321 (1980). Quantitative analysis of cardenolides in latex and leaves of C. procera: eidem, Phytochemistry 21, 2343 (1982). Biosynthesis of labelled compd: M. S. Lee, J. N. Sieber, ibid. 22, 923 (1983).

Lobelanine CAS Registry Number: 579-21-5 山梗烷酮

CAS Name: cis-2,2'-(1-Methyl-2,6-piperidinediyl)bis[1-phenylethanone]
Additional Names: 2,2''-(1-methyl-2,6-piperidinediyl)diacetophenone
Percent Composition: C 78.77%, H 7.51%, N 4.18%, O 9...
Literature References: After lobeline, the most abundant alkaloid of Lobelia inflata L., Lobeliaceae. Isoln: Wieland et al., Ann. 444, 40 (1925). Synthesis: Schöpf, Lehmann, ibid. 518, 1 (1935); Parker et al., J. Chem. Soc. 1959, 2433.

Voglibose CAS Registry Number: 83480-29-9 伏格列波糖

CAS Name: 3,4-Dideoxy-4-[[2-hydroxy-1-(hydroxymethyl)ethyl]amino]-2-C-(hydroxymethyl)-D-epiinositol
Additional Names: N-(1,3-dihydroxy-2-propyl)valiolamineTrademarks: Basen (Takeda)
Percent ...
Literature References: a-Glucosidase inhibitor. Prepn: S. Horii et al., EP 56194; eidem, US 4701559 (1982, 1987 both to Takeda); and structure-activity study: eidem et al., J. Med. Chem. 29, 1038 (1986). Synthesis: H. Fukase, S. Horii, J. Org. Chem. 57, 3651 (1992). Enzyme inhibition and pharmacology: T. Matsuo et al., Am. J. Clin. Nutr. 55, 314S (1992). Clinical pharmacology: B. Göke et al., Digestion 56, 493 (1995). Clinical evaluation in hyperinsulinemia: K. Shinozaki et al., Metabolism 45, 731 (1996).

Miglitol CAS Registry Number: 72432-03-2 米各尼醇

CAS Name: 1,5-Dideoxy-1,5-[(2-hydroxyethyl)imino]-D-glucitol
Additional Names: N-(2-hydroxyethyl)moranoline; (2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)-3,4,5-piperidinetriol; N-(b-hydro...
Literature References: a-Glucosidase inhibitor; hydroxyethyl derivative of 1-deoxynojirimycin, q.v. Prepn: B. Junge et al., DE 2758025; eidem, US 4639436 (1979, 1987 both to Bayer AG). Inhibition of a-glucosidase: B. Lembcke et al., Digestion 31, 120 (1985); and hypoglycemic activity: Y. Yoshikuni et al., J. Pharmacobio-Dyn. 11, 356 (1988). Clinical evaluations in insulin dependent diabetes: J. Gerard et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 25, 483 (1987); F. P. Kennedy, J. E. Gerich, Clin. Pharmacol. Ther. 42, 455 (1987). Review of pharmacology, clinical efficacy, and therapeutic potential in non-insulin dependent diabetes: L. J. Scott, C. M. Spencer, Drugs 59, 521-549 (2000).

Digalogenin CAS Registry Number: 6877-35-6 (3beta,5alpha,15beta,25R)-螺甾烷-3,15-二醇

CAS Name: (3b,5a,15b,25R)-Spirostan-3,15-diol
Percent Composition: C 74.96%, H 10.25%, O 14.79%
Literature References: Aglycon of digalonin. Isoln from saponin mixture and partial synthesis from digitogenin: Tschesche, Wulff, Ber. 94, 2019 (1961).

Diginatigenin CAS Registry Number: 559-57-9

CAS Name: (3b,5b,12b,16b)-3,12,14,16-Tetrahydroxycard-20(22)-enolide
Additional Names: 12-hydroxygitoxigenin; 16-hydroxydigoxigenin
Percent Composition: C 67.96%, H 8.43%, O 23.61%
Literature References: Aglycone of diginatin from Digitalis lanata Ehrk., Scrophulariaceae: Murphy, J. Am. Pharm. Assoc. Sci. Ed. 44, 719 (1955). Aglycone of lanatoside D: Angliker et al., Ann. 607, 131 (1957). Obtained by microbiological conversion of gitoxigenin: Tamm, Gubler, Helv. Chim. Acta 41, 1762 (1958); Okado et al., Chem. Pharm. Bull. 8, 530 (1960). Structure: Linde et al., Helv. Chim. Acta 42, 2040 (1959); Okado et al., Chem. Pharm. Bull. 8, 535 (1960).

Diosmetin CAS Registry Number: 520-34-3 香叶木素

CAS Name: 5,7-Dihydroxy-2-(3-hydroxy-4-methoxyphenyl)-4H-1-benzopyran-4-one
Additional Names: 3',5,7-trihydroxy-4'-methoxyflavone; cyanidenon-4'-methyl ether 1479; luteolin-4'-methyl ether
P...
Literature References: Aglycone of diosmin, q.v. Prepn from diosmin isolated from various plant sources: O. A. Oesterle, G. Wander, Helv. Chim. Acta 8, 519 (1925); isoln from lemons (Citrus limon Linn., Rutaceae): R. M. Horowitz, J. Org. Chem. 21, 1184 (1956). Synthesis and structural elucidation: G. Zemplén, R. Bognár, Ber. 76, 452 (1943). Synthesis: A. Lovecy et al., J. Chem. Soc. 1930, 817; N. B. Lorette et al., J. Org. Chem. 16, 930 (1951); J. H. Looker, M. J. Holm, ibid. 24, 1019 (1959). HPLC determn in biological fluids: D. Baylocq et al., Ann. Pharm. Fr. 41, 115 (1983).

Diosgenin CAS Registry Number: 512-04-9 薯蓣皂苷元

CAS Name: (3b,25R)-Spirost-5-en-3-ol
Additional Names: nitogenin
Percent Composition: C 78.21%, H 10.21%, O 11.58%
Literature References: Aglycone of saponin dioscin. From Dioscorea tokoro Makino, Dioscoreaceae: Tsukamoto, J. Pharm. Soc. Jpn. 56, 135 (1936); from rhizomes of Trillium erectum L., Liliaceae and D. villosa L., Dioscoreaceae: Marker et al., J. Am. Chem. Soc. 62, 2542 (1940). Plant sources for diosgenin: Marker et al., ibid. 65, 1199 (1943); Wall et al., J. Am. Pharm. Assoc. Sci. Ed. 46, 653 (1957). Identity with nitogenin: Marker et al., J. Am. Chem. Soc. 65, 1248 (1943). Structure: Marker et al., ibid. 62, 2525 (1940). Configuration at C25: James, J. Chem. Soc. 1955, 637. Synthesis: Mazur et al., J. Am. Chem. Soc. 82, 5889 (1960); Kessar et al., Tetrahedron Lett. 1966, 4319. Obtained commercially from Dioscorea composita Hemsl. and D. terpinapensis Uline (see under Barbasco). Isoln from barbasco varieties: Julian, US 3019220 (1962 to Julian Labs.).