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

Chlorisondamine Chloride CAS Registry Number: 69-27-2 二碘化氯异吲哚铵

CAS Name: 4,5,6,7-Tetrachloro-2,3-dihydro-2-methyl-2-[2-(trimethylammonio)ethyl]-2H-isoindolium dichloride
Additional Names: 4,5,6,7-tetrachloro-2-(2-dimethylaminoethyl)-2-methylisoindolinium c...
Literature References: Nicotinic receptor antagonist of the ganglion blocking class. Prepn: Allen, Ocampo, J. Electrochem. Soc. 103, 452, 682 (1956); Huebner, US 3025294 (1962 to Ciba). Pharmacology: P. B. S. Clarke et al., Br. J. Pharmacol. 111, 397 (1994). Use in studies of neuronal nicotinic acetylcholine receptors: A. S. Woods et al., J. Proteome Res. 2, 207 (2003).

Nitroglycerin CAS Registry Number: 55-63-0 硝酸甘油

CAS Name: 1,2,3-Propanetriol trinitrate
Additional Names: glyceryl trinitrate; glycerol nitric acid triester; nitroglycerol; trinitroglycerol; glonoin; trinitrin; blasting gelatin; blasting oil...
Literature References: Nitric oxide donor that induces vasodilation. Prepn: Sobrero, Ann. 64, 398 (1847); Williamson, Ann. 92, 305 (1854). Review of the early literature: J. W. Lawrie, Glycerol and the Glycols (New York, 1928). Review of chemistry and biochemistry: F. J. DiCarlo, Drug Metab. Rev. 4, 1-38 (1975). Review of mechanism of action: S. F. Vatner, G. R. Heyndrickx, Handb. Exp. Pharmakol. 40, 131-161 (1975). Molecular mechanism of nitric oxide release: Z. Chen et al., Proc. Natl. Acad. Sci. USA 99, 8306 (2002). Review of the first hundred years: J. R. Parratt, J. Pharm. Pharmacol. 31, 801-809 (1979). Comprehensive description: E. F. McNiff et al., Anal. Profiles Drug Subs. 9, 519-541 (1980). Symposium on nitroglycerin therapy, perspectives and mechanisms: Am. J. Med. 74, no. 6B, 1-94 (1983). Review of pharmacology and clinical studies of intravenous administration in heart disease: E. M. Sorkin et al., Drugs 27, 45 (1984). Clinical trial in treatment of anal fissures: J. H. Scholefield et al., Gut 52, 264 (2005).

N G -Methylarginine CAS Registry Number: 17035-90-4 Nω-单甲基-L-精氨酸乙酸酯

CAS Name: N5-[Imino(methylamino)methyl]-L-ornithine
Additional Names: tilarginine; targinine; NG-monomethyl-L-arginine; L-NMA
Percent Composition: C 44.67%, H 8.57%, N 29.77%, O 17.00%
Literature References: Nitric oxide synthase (NOS) inhibitor; naturally occurring analog of arginine. Isoln from bovine brain and prepn: T. Nakajima et al., Biochim. Biophys. Acta 230, 212 (1971). Improved prepn: J. L. Corbin, M. Reporter, Anal. Biochem. 57, 310 (1974); S. Pundak, M. Wilchek, J. Org. Chem. 46, 808 (1981); of acetate salt: W. Zhang et al., Synth. Commun. 24, 2789 (1994). Inhibition of NO release by endothelial cells: R. M. J. Palmer et al., Biochem. Biophys. Res. Commun. 153, 1251 (1988). Review of biological significance: J. Leiper, P. Vallance, Cardiovasc. Res. 43, 542-548 (1999). Clinical evaluation in cardiogenic shock: G. Cotter et al., Circulation 101, 1358 (2000).

Nitroakridin 3582 CAS Registry Number: 6035-39-8 2-丙醇,1-(二乙胺基)-3-[(2,3-二甲氧基-6-硝基-9-虄啶基)氨基]-

CAS Name: 1-Diethylamino-3-[(2,3-dimethoxy-6-nitro-9-acridinyl)amino]-2-propanol
Additional Names: 5-(g-diethylamino-b-hydroxypropyl)amino-2-nitro-7,8-dimethoxyacridine; 9-(3-diethylamino-2-hyd...
Literature References: Nitroacridine dye with antimicrobial activity. Prepn: Bockmühl, Fehrle, US 2040070 (1936 to Winthrop); BIOS Final Report No. 766 (1946); Miller, Wagner, J. Org. Chem. 13, 891 (1948); Steck et al., J. Am. Chem. Soc. 79, 4414 (1957). Exptl use for in vitro identification of hypoxic cells: A. C. Begg et al., Br. J. Radiol. 56, 970 (1983).

Chlorambucil CAS Registry Number: 305-03-3 苯丁酸氮芥

CAS Name: 4-[Bis(2-chloroethyl)amino]benzenebutanoic acid
Additional Names: 4-[p-[bis(2-chloroethyl)amino]phenyl]butyric acid; g-[p-di(2-chloroethyl)aminophenyl]butyric acid; N,N-di-2-chloroeth...
Literature References: Nitrogen mustard deriv. Prepn: W. C. J. Ross et al., GB 727336; eidem, US 2944079 (1955, 1960 both to Nat. Res. Dev. Corp.); Everett et al., J. Chem. Soc. 1953, 2390. Improved process: Phillips, Mentha, US 3046301 (1962 to Burroughs Wellcome). Chemotherapeutic activity: Van Putten et al., Eur. J. Cancer 7, 11 (1971). Toxicity: W. C. J. Ross, Biochem. Pharmacol. 13, 969 (1964). Review of carcinogenicity studies: IARC Monographs 9, 125-134 (1975). Comprehensive description: M. Tariq, A. A. Al-Badr, Anal. Profiles Drug Subs. 16, 85-118 (1987).

Trichlormethine CAS Registry Number: 555-77-1 三(2-氯乙基)胺

CAS Name: 2-Chloro-N,N-bis(2-chloroethyl)ethanamine
Additional Names: 2,2',2''-trichlorotriethylamine; tris(b-chloroethyl)amine; trimustinePercent Composition: C 35.23%, H 5.91%, Cl 52.00%, N 6...
Literature References: Nitrogen mustard formerly used as a chemical warfare agent. Prepd by the action of thionyl chloride on triethanolamine: Ward, J. Am. Chem. Soc. 57, 914 (1935); US 2072348 (1937 to Hercules Powder). Improved procedure: Wilson, Tishler, J. Am. Chem. Soc. 73, 3635 (1951); Witten in Kirk-Othmer Encyclopedia of Chemical Technology vol. 7 (Interscience, New York, 1951) p 130. Clinical use in treatment of Hodgkin's disease and leukemias: L. S. Goodman et al., J. Am. Med. Assoc. 132, 126 (1946). Evaluation of carcinogenic risk: IARC Monographs 50, 143 (1990). GC determn in air: J. R. Stuff et al., J. Chromatogr. A 849, 529 (1999).

Canfosfamide CAS Registry Number: 158382-37-7 (2R)-L-gamma-谷氨酰-3-((2-((二(二(2-氯乙基)氨基)亚膦酰)氧基)乙基)磺酰基)-L-丙氨酰-2-苯基甘氨酸

CAS Name: (2R)-L-g-Glutamyl-3-[[2-[[bis[bis(2-chloroethyl)amino]phosphinyl]oxy]ethyl]sulfonyl]-L-alanyl-2-phenylglycine
Additional Names: g-glutamyl-a-amino-b-((2-ethyl-N,N,N',N'-tetrakis(2-chl...
Literature References: Nitrogen mustard prodrug preferentially activated by glutathione S-transferase P1-1. Prepn: M. H. Lyttle et al., J. Med. Chem. 37, 1501 (1994); L. M. Kauvar et al., WO 9509866; eidem, US 5556942 (1995, 1996 both to Terrapin). Mechanism of activation: A. Satyam et al., J. Med. Chem. 39, 1736 (1996). In vitro and in vivo antitumor and myelosuppressive effects: A. S. Morgan et al., Cancer Res. 58, 2568 (1998). Clinical pharmacokinetics and toxicology in advanced solid malignancies: L. S. Rosen et al., Clin. Cancer Res. 9, 1628 (2003); idem et al., ibid. 10, 3689 (2004).

Bakankosin CAS Registry Number: 1398-17-0 (3S)-4a-乙烯基-3-beta-D-吡喃葡萄糖基氧基-3,4,4abeta,5,6,7-六氢-8H-吡喃并[3,4-c]吡啶-8-酮

CAS Name: [3S-(3a,4b,4aa)]-4-Ethenyl-3-(b-D-glucopyranosyloxy)-3,4,4a,5,6,7-hexahydro-8H-pyrano[3,4-c]pyridin-8-one
Additional Names: bacancosin
Trademarks: Bakankoside
Percent Compositio...
Literature References: Nitrogenous glucoside from seed of Strychnos vacacoua Baill., Loganiaceae. Ref: E. Bourquelot, H. Hérissey, Compt. Rend. 144, 575 (1907); 147, 750 (1908); Arch. Pharm. 247, 56 (1909); K. Balenovic et al., Helv. Chim. Acta 35, 2519 (1952). Proposed structure: G. Büchi, R. E. Manning, Tetrahedron Letters no. 26, 5 (1960); H. C. Beyerman et al., Bull. Soc. Chim. Fr. 1961, 1812; H. Inouye et al., Chem. Pharm. Bull. 24, 1406 (1976). Synthesis and structure: L. F. Tietze, Tetrahedron Lett. 29, 2535 (1976).

Disufenton CAS Registry Number: 168021-77-0

CAS Name: 4-[[(1,1-Dimethylethyl)oxidoimino]methyl]-1,3-benzenedisulfonic acid
Additional Names: 2,4-disulfonyl-a-phenyl-tert-butylnitrone
Percent Composition: C 39.16%, H 4.48%, N 4.15%, O ...
Literature References: Nitrone-based spin trapping agent; derivative of PBN, q.v. Prepn: J. M. Carney, WO 9517876; idem, US 5488145 (1995, 1996 both to Oklahoma Med. Res. Found.). Pharmacology: S. Kuroda et al., J. Cereb. Blood Flow Metab. 19, 778 (1999). Comparative radical trapping study: K. R. Maples et al., Free Radical Res. 34, 417 (2001). Clinical pharmacokinetics: K. R. Lees et al., Stroke 32, 675 (2001). Clinical trial in acute ischemic stroke: idem et al., N. Engl. J. Med. 354, 588 (2006). Reviews of pharmacology and therapeutic potential: P. A. Lapchak, Curr. Opin. Invest. Drugs 3, 1758-1762 (2002); P. A. Lapchak, D. M. Araujo, CNS Drug Rev. 9, 253-262 (2003).

Dexanabinol CAS Registry Number: 112924-45-5 1,1-二甲基庚基-11-羟基四氢大麻酚

CAS Name: (6aS,10aS)-3-(1,1-Dimethylheptyl)-6a,7,10,10a-tetrahydro-1-hydroxy-6,6-dimethyl-6H-dibenzo[b,d]pyran-9-methanol
Additional Names: (+)-(3S,4S)-7-hydroxy-D6-tetrahydrocannabinol-1,1-dim...
Literature References: NMDA antagonist. Nonpsychotropic derivative of tetrahydrocannabinol, q.v. Prepn: R. Mechoulam et al., DE 3735990; eidem, US 4876276 (1988, 1989 both to Yissum Res. Dev. Co.); R. Mechoulam et al., Tetrahedron: Asymmetry 1, 315 (1990). Cannabinoid receptor binding study: A. C. Howlett et al., Neuropharmacology 29, 161 (1990). Inhibition of nuclear factor-kB (NF-kB): E. Jüttler et al., Neuropharmacology 47, 580 (2004). Pharmacology: N. Eshhar et al., Eur. J. Pharmacol. 283, 19 (1995). Clinical pharmacokinetics: M. E. Brewster et al., Int. J. Clin. Pharmacol. Ther. 35, 361 (1995). Clinical evaluation in severe head injury: N. Knoller et al., Crit. Care Med. 30, 548 (2002).