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

Mitoxantrone CAS Registry Number: 65271-80-9 米托蒽醌

CAS Name: 1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione
Additional Names: DHAQPercent Composition: C 59.45%, H 6.35%, N 12.61%, O 21.60%
Literature References: Immunosuppressive and cytostatic anthracenedione. Prepn: R. K. Y. Zee-Cheng, C. C. Cheng, J. Med. Chem. 21, 291 (1978); K. C. Murdock et al., ibid. 22, 1024 (1979); eidem, DE 2835661; K. C. Murdock, F. E. Durr, US 4197249 (1979, 1980 both to Am. Cyanamid). Antitumor activity: R. E. Wallace et al., Cancer Res. 39, 1570 (1979). HPLC determn in plasma: K. T. Lin et al., J. Chromatogr. 465, 75 (1989). Comprehensive description: J. H. Beijnen et al., Anal. Profiles Drug Subs. 17, 221-258 (1988). Review of toxicology: M. McDonald et al., Drugs Exp. Clin. Res. 10, 745-752 (1984); of pharmacology and clinical efficacy in cancer: J. Koeller, M. Eble, Clin. Pharm. 7, 574-581 (1988); of pharmacokinetics and metabolism: G. Ehninger et al., Clin. Pharmacokinet. 18, 365-380 (1990). Review of pharmacology and clinical efficacy in multiple sclerosis: K. K. Jain, Expert Opin. Invest. Drugs 9, 1139-1149 (2000).

Azathioprine CAS Registry Number: 446-86-6 硫唑嘌呤

CAS Name: 6-[(1-Methyl-4-nitro-1H-imidazol-5-yl)thio]-1H-purine
Additional Names: 6-(1-methyl-4-nitro-5-imidazolyl)mercaptopurine; azothioprineTrademarks: Azanin (Tanabe); Imuran (GSK); Imurek ...
Literature References: Immunosuppressive antimetabolite; also active as disease modifying antirheumatic drug (DMARD). Metabolized in vivo to 6-mercaptopurine, q.v. Prepn: G. H. Hitchings, G. B. Elion, US 3056785 (1962 to Burroughs Wellcome). Metabolism and pharmacokinetics: T. L. Ding, L. Z. Benet, Drug Metab. Dispos. 7, 373 (1979). Carcinogenicity studies: P. S. Mitrou et al., Arzneim.-Forsch. 29, 483, 662 (1979). HPLC determn in plasma: E. C. Van Os et al., J. Chromatogr. B 679, 147 (1996). Clinical trial in rheumatoid arthritis: R. F. Wilkens, D. Stablein, J. Rheumatol. 23, Suppl. 44, 64 (1996). Comprehensive description: W. P. Wilson, S. A. Benezra, Anal. Profiles Drug Subs. 10, 29-53 (1981). Review of clinical efficacy in renal transplantation: G. L. C. Chan et al., Pharmacotherapy 7, 165-177 (1987); in multiple sclerosis: C. Confavreux, T. Moreau, Mult. Scler. 1, 379-384 (1996); in inflammatory bowel disease: W. J. Sandborn, Scand. J. Gastroenterol. 33, Suppl. 225, 92-99 (1998).

Eicosapentaenoic Acid CAS Registry Number: 10417-94-4 顺式-5,8,11,14,17-二十碳五烯酸

CAS Name: (5Z,8Z,11Z,14Z,17Z)-5,8,11,14,17-Eicosapentaenoic acid
Additional Names: (all-Z)-5,8,11,14,17-eicosapentaenoic acid; all-cis-fatty acid 20:5 omega-3; EPA; icosapent
Percent Composi...
Literature References: Important polyunsaturated fatty acid of the marine food chain that serves as a precursor for the prostaglandin-3 and thromboxane-3 families. It differs from arachidonic acid, q.v. (the eicosatetraenoic acid that is a precursor for the prostaglandin and thromboxane-2 families) by the extra double bond between the third and fourth carbons from the "methyl end" of the molecule. Isoln from cod liver oil: E. Klenk, D. Eberhagen, Z. Physiol. Chem. 307, 42 (1957). Enzymatic conversion to prostaglandin E3: S. Bergström et al., J. Biol. Chem. 239, PC 4006 (1964). Effects on role of platelets in thrombosis: K. C. Srivastava et al., Biochem. Exp. Biol. 16, 317 (1980). Effects on prostacyclin-like material in human umbilical vasculature: J. Dyerberg, K. A. Jorgensen, Artery 8, 12 (1980). A possible relationship between diets rich in EPA in marine oils and low rates of ischemic heart disease has been proposed: H. O. Bang et al., Am. J. Clin. Nutr. 33, 2657 (1980); J. Dyerberg, Philos. Trans. R. Soc. London Ser. B 294, 373 (1981). Clinical evaluation of lipid lowering effect: Y. Nagakawa et al., Atherosclerosis 47, 71 (1983); of use in rheumatoid arthritis: J. M. Kremer et al., Ann. Intern. Med. 106, 497 (1987); of use in Raynaud's phenomenon: R. A. DiGiacomo et al., Am. J. Med. 86, 158 (1989).

SAICAR CAS Registry Number: 3031-95-6 (2S)-2-[[5-氨基-1-[(2R,3R,4S,5R)-3,4-二羟基-5-(膦酰氧基甲基)四氢呋喃-2-基]咪唑-4-羰基]氨基]丁二酸

CAS Name: N-[[5-Amino-1-(5-O-phosphono-b-D-ribofuranosyl)-1H-imidazol-4-yl]carbonyl]-L-aspartic acid
Additional Names: N-[(5-amino-1-ribofuranosylimidazol-4-yl)carbonyl]aspartic acid 5'-phospha...
Literature References: Important purine precursor. Synthesis by enzymic reaction according to the equation AIR + ATP + aspartic acid + CO2 ® SAICAR + ADP + orthophosphate: Lukens, Buchanan, J. Biol. Chem. 234, 1791 (1959). Production by adenine-requiring mutants of Bacillus subtilis: Ohmura et al., US 3280007 (1966 to Takeda). Synthesis of SAICAR and derivatives: Burrows, Shaw, J. Chem. Soc. C 1967, 1088; Burrows et al., ibid. 1968, 40.

Anabasine CAS Registry Number: 494-52-0 (-)-假木贼碱

CAS Name: 3-(2-Piperidinyl)pyridine
Additional Names: 2-(3-pyridyl)piperidine; neonicotine
Percent Composition: C 74.04%, H 8.70%, N 17.27%
Literature References: In Anabasis aphylla L., Chenopodiaceae: Orechoff, Menschikoff, Ber. 64, 266 (1931); in Nicotiana glauca Graham, Solanaceae: Smith, J. Am. Chem. Soc. 57, 959 (1935); Pyriki, Oehler, Pharmazie 9, 685 (1954). Synthesis: Späth, Ber. 70B, 70 (1937). Extracted on a large scale in Russia. Industrial extraction processes: Sadykov, Timbekov, J. Appl. Chem. USSR 29, 148 (1956). Abs config: Lukes et al., Collect. Czech. Chem. Commun. 27, 751 (1962).

Cupreine CAS Registry Number: 524-63-0 (8α,9R)-奎宁-6',9-二醇

CAS Name: (8a,9R)-Cinchonan-6',9-diol
Additional Names: hydroxycinchonidine; ultraquinine
Percent Composition: C 73.52%, H 7.14%, N 9.03%, O 10.31%
Literature References: In bark and seeds of Remijia pedunculata Flueck., Rubiaceae. Isoln: Howard, Hodgkin, J. Chem. Soc. 41, 16 (1882). Separated from homoquinine by treatment with NaOH: Hesse, Ann. 230, 55 (1885). Reduction to hydrocupreine: Giemsa, Halberkann, Ber. 51, 1325 (1918). Conversion into cinchonidine: King, J. Chem. Soc. 1946, 523.

Actinodaphnine CAS Registry Number: 517-69-1 放线瑞香宁

CAS Name: 6,7,7a,8-Tetrahydro-11-methoxy-5H-benzo[g]-1,3-benzodioxolo[6,5,4-de]quinolin-10-ol
Additional Names: 10-methoxy-1,2-(methylenedioxy)-6aa-noraporphin-9-ol; 1,2-methylenedioxy-9-hydrox...
Literature References: In bark of Actinodaphne hookeri Meissn., Lauraceae. Isoln: Krishna, Ghose, J. Indian Chem. Soc. 9, 429 (1932). Structure: Ghose et al., Helv. Chim. Acta 17, 919 (1934). Photolytic synthesis: M. S. Premila et al., Indian J. Chem. 13, 945 (1975).

Frangulin CAS Registry Number: 60529-33-1

Additional Names: Franguloside; avornin
Trademarks: Cascarin
Literature References: In berries, bark, and rootbark of Rhamnus spp., especially in alder buckthorn (Rhamnus frangula L.), Rhamnus carthartica L., and Rhamnus purshiana DC. (Cascara sagrada), Rhamnaceae. Prepn from bark of alder buckthorn: Bridel, Charaux, Bull. Soc. Chim. Biol. 15, 642 (1933); M. Kubiak, Herba Pol. 23, 217 (1977), C.A. 88, 166260b (1978). Consists of the two glucosides, frangulins A and B, which were originally thought to be isomeric. Structure and synthesis of frangulin A: Hörhammer, Wagner, Z. Naturforsch. 27B, 959 (1972). Structure of frangulin B: Wagner, Demuth, Tetrahedron Lett. 1972, 5013.

Carnegine CAS Registry Number: 490-53-9

CAS Name: 1,2,3,4-Tetrahydro-6,7-dimethoxy-1,2-dimethylisoquinoline
Additional Names: 6,7-dimethoxy-1,2-dimethyl-1,2,3,4-tetrahydroisoquinoline; pectenine
Percent Composition: C 70.56%, H 8....
Literature References: In Carnegiea gigantea (Engelm.) Britt. Rose (Cereus giganteus Engelm.), Cactaceae, a cactus of Arizona and Mexico. Extraction procedure: Heyl, Arch. Pharm. 266, 668 (1928). Synthesis: Späth, Ber. 62, 1021 (1929); Nakada, Nisgihara, J. Pharm. Soc. Jpn. 64, 74 (1944). Pharmacology: E. Santi-Soncin, M. Furlanut, Fitoterapia 43, 21 (1972), C.A. 80, 66667f (1974). Review of synthetic methods: A. B. J. Bracca, T. S. Kaufman, Tetrahedron 60, 10575-10610 (2004).

Cuscohygrine CAS Registry Number: 454-14-8 红古豆碱

CAS Name: 1,3-Bis(1-methyl-2-pyrrolidinyl)-2-propanone
Additional Names: cuskhygrine; bellaradine
Percent Composition: C 69.60%, H 10.78%, N 12.49%, O 7.13%
Literature References: In coca leaves of various origin. Found in crude hygrine. Readily converted to hygrine by acids and bases. Isoln: Liebermann, Ber. 22, 679 (1898); Liebermann, Cybulski, ibid. 28, 578 (1895). Identity with bellaradine: Steinegger, Phokas, Pharm. Acta Helv. 30, 441 (1955). Structure: Hess, Fink, Ber. 53, 794 (1920); Sohl, Shriner, J. Am. Chem. Soc. 55, 3828 (1933); Rapoport, Jorgensen, J. Org. Chem. 14, 664 (1949). Synthesis: Späth, Tuppy, Monatsh. Chem. 79, 119 (1948); Galinovsky et al., ibid. 82, 551 (1951). Enzymatic synthesis: Tuppy, Faltaous, ibid. 91, 167 (1960). Stereochemistry: Galinovsky, Zuber, ibid. 84, 798 (1953). Biosynthesis: E. Leete, Chem. Commun. 1980, 1170.