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

Cysteamine CAS Registry Number: 60-23-1 β-巯基乙胺

CAS Name: 2-Aminoethanethiol
Additional Names: mercaptamine; b-mercaptoethylamine; 2-aminoethyl mercaptan; thioethanolamine; decarboxycysteine; MEA; mercamineTrademarks: Becaptan (Labaz); Lambr...
Literature References: A sulfhydryl compound with a variety of biological effects. Prepn: Gabriel, Leupold, Ber. 31, 2837 (1898); Knorr, Rössler, ibid. 36, 1281 (1903); Mills, Jr., Bogart, J. Am. Chem. Soc. 62, 1173 (1940); Wenker, ibid. 57, 2328 (1935); D. A. Shirley, Preparation of Organic Intermediates (Wiley, New York, 1951) p 189. Use in treatment of paracetamol (acetaminophen) poisoning: L. F. Prescott et al., Lancet 2, 109 (1976); A. L. Harris, Br. Med. J. 284, 825 (1982). Effects in nephropathic cystinosis: M. Yudkoff et al., N. Engl. J. Med. 304, 141 (1981). Radioprotective effects: R. P. Bird, Radiat. Res. 72, 290 (1980); C. J. Koch, R. L. Howell, ibid. 87, 265 (1981). Cysteamine has been shown to be a duodenal ulcerogen in rats: H. Selye, S. Szabo, Nature 244, 458 (1973); S. Szabo, Am. J. Pathol. 93, 273 (1978); P. Kirkegaard et al., Scand. J. Gastroenterol. 15, 621 (1980). Review: S. Szabo, Lab. Invest. 51, 121 (1984). It has also been found to deplete somatostatin concentration: S. Szabo, S. Reichlein, Endocrinology 109, 2255 (1981); S. M. Sagar et al., J. Neurosci. 2, 225 (1982). In pituitary tissue, cysteamine is a potent depletor of prolactin concentrations in vivo and in vitro: W. J. Millard et al., Science 217, 452 (1982). Toxicity studies: E. Beccari et al., Arzneim.-Forsch. 5, 421 (1955); D. L. Klayman et al., J. Med. Chem. 12, 510 (1969); P. K. Srivastava, L. Field, ibid. 18, 798 (1975).

Homocysteine CAS Registry Number: 6027-13-0 L-高半胱氨酸

CAS Name: 2-Amino-4-mercaptobutyric acid
Percent Composition: C 35.54%, H 6.71%, N 10.36%, O 23.67%, S 23.72%
Literature References: A sulfur containing amino acid, produced by the demethylation of methionine and an intermediate in the biosynthesis of cysteine from methionine. Originally obtained from the liver of mammals. Has also been obtained from cystathionine: Binkley, Methods Enzymol. 2, 314 (1955). D-Homocysteine may be prepd from S-benzyl-D-homocysteine, while L-homocysteine is best obtained from L-homocystine: du Vigneaud, Brown, Biochem. Prep. 5, 93 (1957), see also Patterson, du Vigneaud, J. Biol. Chem. 111, 393 (1935); Riegel, du Vigneaud, ibid. 112, 149 (1935). Origin and biochemical conversions in review by Shapiro, Schlenk, Adv. Enzymol. 22, 264-268 (1960). Use of L-form sodium salt as flavor enhancer similar to monosodium glutamate: Kaneko et al., US 3259505 (1966 to Ajinomoto Kabushiki Kaisha).

Cholestyramine Resin CAS Registry Number: 11041-12-6 考来烯胺

Additional Names: ColestyraminTrademarks: Cholybar (Warner-Lambert); Cuemid (Merck Co.); Quantalan (BMS); Questran (BMS)
Literature References: A synthetic, strongly basic anion exchange resin contg quaternary ammonium functional groups which are attached to a styrene-divinylbenzene copolymer. Main constituent: Polystyrene trimethylbenzylammonium as Cl- anion, also contains divinylbenzene. Av polymeric mol wt 106; Cl- content 14-17%. Effect of particle size on bile salt binding capacity: L. M. Hagerman et al., Proc. Soc. Exp. Biol. Med. 139, 248 (1972). Review of pharmacology: H. R. Casdorph in Lipid Pharmacology Vol. 2(2), R. Paoletti, C. J. Glueck, Eds. (Academic Press, New York, 1976) pp 222-256. Clinical evaluation in chlordecone detoxification: W. J. Cohn et al., N. Engl. J. Med. 298, 243 (1978). Review of pharmacology and therapeutic efficacy: M. Ast, W. H. Frishman, J. Clin. Pharmacol. 30, 99-106 (1990).

Alantolactone CAS Registry Number: 546-43-0 土木香内酯

CAS Name: [3aR-(3aa,5b,8ab,9aa)]-3a,5,6,7,8,8a,9,9a-Octahydro-5,8a-dimethyl-3-methylenenaphtho[2,3-b]furan-2(3H)-one
Additional Names: 8b-hydroxy-4aH-eudesm-5-en-12-oic acid g-lactone; helenin;...
Literature References: A terpene from roots of Inula helenium L., Compositae: Kallen, Ber. 6, 1506 (1873); 9, 154 (1876); Ruzicka et al., Helv. Chim. Acta 14, 397, 1090 (1931); 16, 268 (1933). Structure: Marshall, Cohen, J. Org. Chem. 29, 3727 (1964). Stereoselective synthesis: Marshall et al., J. Am. Chem. Soc. 88, 3408 (1966).

Tiamenidine CAS Registry Number: 31428-61-2 噻美尼定.

CAS Name: N-(2-Chloro-4-methyl-3-thienyl)-4,5-dihydro-1H-imidazol-2-amine
Additional Names: 2-[(2-chloro-4-methyl-3-thienyl)amino]-2-imidazoline; 2-chloro-4-methyl-3-(2'-imidazolin-2'-ylamino)t...
Literature References: A thiophene analog of clonidine, q.v. Prepn: R. Rippel et al., DE 1941761; eidem, US 3758476 (1971, 1973, both to Hoechst). Structural studies: J. M. Leger, C.R. Seances Acad. Sci. Ser. C 289, 93 (1979); A. Carpy et al., Mol. Pharmacol. 21, 400 (1981). GC mass spectrometry determn in human plasma: T. A. Bryce, J. L. Burrows, Biomed. Mass Spectrom. 6, 27 (1979). Pharmacology: E. Lindner, J. Kaiser, Arch. Int. Pharmacodyn. Ther. 211, 305 (1974). Activity as a-adrenoceptor agonist: A. G. Roach et al., J. Pharmacol. Exp. Ther. 227, 421 (1983).

Patchouli Alcohol CAS Registry Number: 5986-55-0 百秋李醇

CAS Name: [1R-(1a,4b,4aa,6b,8aa)]-Octahydro-4,8a,9,9-tetramethyl-1,6-methanonaphthalen-1(2H)-ol
Additional Names: patchouli camphor
Percent Composition: C 81.02%, H 11.79%, O 7.19%
Literature References: A tricyclic sesquiterpene alcohol isolated from oil of patchouli: Gadamer, Amenomiya, Arch. Pharm. 241, 39 (1903). Proposed structure: Treibs, Ann. 564, 141 (1949). Revised structure: Dobler et al., Proc. Chem. Soc. London 1963, 383. Structural studies: Büchi et al., J. Am. Chem. Soc. 78, 1262 (1956); 83, 927 (1961); 84, 3205 (1962); 86, 4438 (1964). Synthesis of dl-form: Danishevsky, Dumas, Chem. Commun. 1968, 1287; Mirrington, Schmalzl, J. Org. Chem. 37, 2871 (1972); K. Yamada et al., Tetrahedron 35, 293 (1979). Stereoselective total synthesis of racemic form: F. Näf, G. Ohloff, Helv. Chim. Acta 57, 1868 (1974); of natural, racemic and (+)-forms: F. Näf et al., ibid. 64, 1387 (1981). Review: Walker, Manuf. Chem. Aerosol News 39, no. 7, 27 (1968).

Procerin CAS Registry Number: 552-96-5

CAS Name: 2-Hydroxy-5-(3-methyl-2-butenyl)-4-(1-methylethenyl)-2,4,6-cycloheptatrien-1-one
Percent Composition: C 78.23%, H 7.88%, O 13.89%
Literature References: A tropolone isolated from Juniperus procera Hochst., Cupressaceae, obtained in Kenya: Petterson, Runeberg, Acta Chem. Scand. 15, 713 (1961). Structure: Runeberg, ibid. 645. Synthesis: Kitahara, Kato, Bull. Chem. Soc. Jpn. 37, 895 (1964).

Linatine CAS Registry Number: 10139-06-7 gamma-谷氨酰-1-氨基-D-脯氨酸

CAS Name: 1-[(4-Amino-4-carboxy-1-oxobutyl)amino]-D-proline
Additional Names: N-(D-2-carboxy-1-pyrrolidinyl)-L-glutamine; 1-[N-(g-L-glutamyl)amino]-D-proline
Percent Composition: C 46.33%, H...
Literature References: A vitamin B6 antagonist. The first reported naturally occurring hydrazino acid having antibacterial properties. Isoln from flaxseed (Linum usitatissimum), characterization, and synthesis: Klosterman et al., Biochemistry 6, 170 (1967); Lamoureux, Diss. Abstr. B 28, 4908 (1968). Bacterial inhibition: Parsons et al., Antimicrob. Agents Chemother. 1967, 415.

Succimer CAS Registry Number: 304-55-2 2,3-二巯基丁二酸

CAS Name: (2R,3S)-rel-2,3-Dimercaptobutanedioic acid
Additional Names: meso-2,3-dimercaptosuccinic acid; DMS; DMSATrademarks: Chemet (McNeil)
Percent Composition: C 26.37%, H 3.32%, O 35.12%...
Literature References: A water soluble chelating agent. Prepn: L. N. Owen, M. U. S. Sultanbawa, J. Chem. Soc. 1949, 3109. Pharmacology, toxicity and activity in heavy metal poisoning in animals: E. Friedheim, C. Corvi, J. Pharm. Pharmacol. 27, 624 (1975); J. H. Graziano et al., J. Pharmacol. Exp. Ther. 207, 1051 (1978). GC determn in urine: J. J. Knudsen, E. L. McGown, J. Chromatogr. 424, 231 (1988). Clinical evaluations in heavy metal poisoning: E. Friedheim et al., Lancet 2, 1234 (1978); L. Fournier et al., Med. Toxicol. 3, 499 (1988). Diagnostic use of complex with technetium in urinary tract imaging: I. G. Verber et al., Arch. Dis. Child. 63, 1320 (1988); in tumor imaging: H. Ohta et al., Nucl. Med. Commun. 9, 105 (1988). Review: H. V. Aposhian, "Biological Chelation: 2,3-Dimercaptopropanesulfonic Acid and Meso-Dimercaptosuccinic Acid" in Adv. Enzyme Regul. 20, G. Weber, Ed. (Pergamon Press, Oxford, 1982) pp 301-319. Review of pharmacology and clinical use in heavy metal poisoning: idem, Annu. Rev. Pharmacol. Toxicol. 23, 193-215 (1983); J. H. Graziano, Med. Toxicol. 1, 155-162 (1986).

Epoxomicin CAS Registry Number: 134381-21-8 环氧酶素

CAS Name: N-Acetyl-N-methyl-L-isoleucyl-L-isoleucyl-N-[(1S)-3-methyl-1[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-threoninamide
Additional Names: BU-4061T
Percent Composition: C 60.63%, H 9.09...
Literature References: a¢,b¢-epoxyketone peptide which specifically inhibits proteasome activity. Isoln from actinomycetes: M. Konishi et al., EP 411660; eidem, US 5071957 (both 1991 to Bristol-Myers); and characterization: M. Hanada et al., J. Antibiot. 45, 1746 (1992). Total synthesis: N. Sin et al., Bioorg. Med. Chem. Lett. 9, 2283 (1999). Proteasome selectivity and antiinflammatory activity: L. Meng et al., Proc. Natl. Acad. Sci. USA 96, 10403 (1999). Crystal structure and mechanism of selectivity: M. Groll et al., J. Am. Chem. Soc. 122, 1237 (2000). Use as inhibitor to modulate antigen presentation: K. Schwarz et al., J. Immunol. 164, 6147 (2000).