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

Tricarballylic Acid CAS Registry Number: 99-14-9 1,2,3-丙烷三甲酸

CAS Name: 1,2,3-Propanetricarboxylic acid
Additional Names: b-carboxyglutaric acid
Percent Composition: C 40.92%, H 4.58%, O 54.51%
Literature References: Natural product produced by rumen bacteria; structural component of fumonisin mycotoxins. Prepn from aconitic acid by reduction with sodium amalgam: Fittig, Ann. 314, 15 (1901); by hydrolysis of ethyl propane-1,1,2,3-tetracarboxylate: Clarke, Murray, Org. Synth. coll. vol. I (2nd ed., 1941) p 523. Absorption spectrum: Bielecki, Henri, Ber. 46, 2596 (1913). Crystal structure: J. C. Barnes, J. D. Paton, Acta Crystallogr. C44, 758 (1988). Production by rumen microorganisms: J. B. Russell, N. Forsberg, Br. J. Nutr. 56, 153 (1986). Review of chemistry: A. S. H. Elgazwy, Curr. Org. Chem. 8, 1405-1423 (2004).

Camphor CAS Registry Number: 76-22-2 (±)-樟脑(合成)

CAS Name: 1,7,7-Trimethylbicyclo[2.2.1]heptan-2-one
Additional Names: 2-bornanone; 2-camphanone; 2-keto-1,7,7-trimethylnorcamphane; gum camphor; Japan camphor; Formosa camphor; laurel camphor Literature References: Naturally occuring in both the d- and l-forms; orginally obtained commercially as the d-form from the camphor tree, Cinnamomum camphora T. Nees Ebermeier, Lauraceae. Primarily manufactured from pinene as the racemate. History of isolation and production of natural and synthetic forms: I. Gubelmann, H. W. Elley, Ind. Eng. Chem. 26, 589 (1934); J. M. Derfer, M. M. Derfer in Kirk-Othmer Encyclopedia of Chemical Technology vol. 23 (John Wiley Sons, New York, 4th ed., 1997) pp 865-866. Enantiomeric composition in oils of coriander, sage, and basil: F. Tateo et al., Anal. Commun. 36, 149 (1999). GC determn in human plasma: J. S. Valdez et al., J. Chromatogr. B 729, 163 (1999); in pharmaceutical formulation: E. Gonzálea-Penas et al., Chromatographia 52, 245 (2000). Review: Camphor and Camphor Containing Products (PB293503, 1979) 65 pp; J. S. Mossa, M. M. A. Hassan, Anal. Profiles Drug Subs. 13, 28-93 (1984). Review of use as starting material for syntheses: T. Money, Org. Synth. 3, 1-83 (1996).

Picolinic Acid CAS Registry Number: 98-98-6 2-吡啶甲酸

CAS Name: 2-Pyridinecarboxylic acid
Additional Names: o-pyridinecarboxylic acid
Percent Composition: C 58.54%, H 4.09%, N 11.38%, O 25.99%
Literature References: Naturally occuring isomer of nicotinic acid; by-product of tryptophan catabolism. Prepn: Singer, McElvain, Org. Synth. coll. vol. III, 740 (1955). Review: Oliveto, "Pyridinecarboxylic Acids" in Pyridine and Its Derivatives Part 3, E. Klingsberg, Ed. (Interscience, New York, 1962) p 179. Review of immunobiology and effect on macrophage activation: G. Melillo et al., Adv. Exp. Med. Biol. 398, 135-141 (1996). HPLC determn in biological fluids: C. Dazzi et al., J. Chromatogr. B 751, 61 (2001).

n-Docosanol CAS Registry Number: 661-19-8 正二十二醇

CAS Name: 1-Docosanol
Additional Names: behenic alcohol; behenyl alcohol; docosyl alcohol
Trademarks: Abreva (GSK); Lidakol (Avanir)
Percent Composition: C 80.90%, H 14.20%, O 4.90%
Literature References: Naturally occurring alcohol; active principal of Pygeum africanum extract, q.v., that has been used to treat benign prostatic hypertrophy (BPH). Prepn: R. Willstätter, E. W. Mayer, Ber. 41, 1475 (1908); P. A. Levene, F. A. Taylor, J. Biol. Chem. 59, 905 (1924). Surface thermodynamic properties: S. Pathak, S. S. Katti, J. Chem. Eng. Data 14, 359 (1969). GC-MS determn in Pygeum africanum extract: N. Pierini et al., Boll. Chim. Farm. 121, 27 (1982). Antiviral activity: D. H Katz et al., Ann. N.Y. Acad. Sci. 724, 472 (1994). Study of mechanism of action in BPH: J. Müntzing et al., Invest. Urol. 17, 176 (1979); vs herpes simplex virus: L. E. Pope et al., Antiviral Res. 40, 85 (1998). Clinical evaluation in recurrent herpes labialis: L. Habbema et al., Acta Derm. Venereol. 76, 479 (1996).

Selenocysteine CAS Registry Number: 10236-58-5 硒代-L-半胱氨酸

CAS Name: 3-Selenyl-L-alanine
Additional Names: selenium cysteine
Percent Composition: C 21.44%, H 4.20%, N 8.33%, O 19.04%, Se 46.99%
Literature References: Naturally occurring amino acid found in the active site of certain prokaryotic and eukaryotic enzymes. Highly oxidizable making synthesis difficult. Easily prepared from its oxidized form selenocystine. Prepn of dl-selenocystine: A. Fredga, Sven. Kem. Tidskr. 48, 160 (1936); E. P. Painter, J. Chem. Soc. 69, 229 (1947); of l-form: H. Tanaka, K. Soda, Methods Enzymol. 143, 240 (1987). Reduction of selenocystine and separation of L-selenocysteine: J. N. Burnell et al., J. Inorg. Biochem. 12, 343 (1980). Chemical properties: R. E. Huber, R. S. Criddle, Arch. Biochem. Biophys. 122, 164 (1967). Determn by HPLC/MS: H. E. Ganther et al., Methods Enzymol. 107, 582 (1984); colorimetric determn: N. Esaki, K. Soda, ibid. 143, 148 (1987). Identification of Se as a component in protein: S.-H. Oh et al., Biochemistry 13, 1825 (1974). Characterization of selenocysteine as the Se containing amino acid moiety in various enzymes: J. E. Cone et al., Proc. Natl. Acad. Sci. USA 73, 2659 (1976); J. B. Jones et al., Arch. Biochem. Biophys. 195, 255 (1979); presence in the catalytic site of mammalian glutathione peroxidase: J. W. Forstrom et al., Biochemistry 17, 2639 (1978); J. J. Zabrowski et al., Biochem. Biophys. Res. Commun. 84, 248 (1978). Metabolism in animals: H. Tanaka et al., Curr. Top. Cell. Regul. 27, 487 (1985). Identification of selenocysteine-specific tRNA: W. C. Hawkes et al., Biochim. Biophys. Acta 699, 183 (1982); W. Leinfelder et al., Nature 331, 723 (1988). Review: T. C. Stadtman, FASEB J. 1, 375-379 (1987).

d -Aminolevulinic Acid CAS Registry Number: 106-60-5 5-氨基乙酰丙酸

CAS Name: 5-Amino-4-oxopentanoic acid
Additional Names: ALA
Percent Composition: C 45.80%, H 6.92%, N 10.68%, O 36.60%
Literature References: Naturally occurring amino acid; precursor of tetrapyrroles in the biosynthesis of chlorophyll and heme. Prepn: R. W. Wynn, A. H. Corwin, J. Org. Chem. 15, 203 (1950); A. A. Marei, R. H. Raphael, J. Chem. Soc. 1958, 2624; C. Herdeis, A. Dimmerlung, Arch. Pharm. 317, 304 (1984). Role in tetrapyrrole biosynthesis: D. Shemin, C. S. Russell, J. Am. Chem. Soc. 75, 4873 (1953). Enhancement of chlorophyll formation: E. C. Sisler, W. H. Klein, Physiol. Plant. 16, 315 (1963). HPLC determn in plasma: K. Miyajima et al., J. Chromatogr. B 654, 165 (1994). Review of role in chlorophyll biosynthesis and potential as photodynamic herbicide: C. A. Rebeiz et al., Enzyme Microb. Technol. 6, 390-401 (1984). Review of role in heme biosynthesis and clinical experience in photodynamic therapy: Q. Peng et al., Cancer 79, 2282-2308 (1997).

Bergapten CAS Registry Number: 484-20-8 佛手柑内酯

CAS Name: 4-Methoxy-7H-furo[3,2-g][1]benzopyran-7-one
Additional Names: 5-methoxypsoralen; bergaptan; bergaptene; heraclin; majudin; 5-MOP
Trademarks: Psoraderm-5 (Sunlife)
Percent Compos...
Literature References: Naturally occurring analog of psoralen and isomer of methoxsalen, q.q.v., found in a wide variety of plants. It was first isolated from oil of bergamot from Citrus bergamia Risso, Aurantiodiae: Pomeranz, Monatsh. Chem. 12, 379 (1891), 14, 28 (1893). Isoln from Fagara xanthoxyloides Lam., Rutaceae: H. Thoms, E. Baetcke, Ber. 44, 3326 (1911); 45, 3705 (1912). Synthesis: E. Späth et al., Ber. 70, 478 (1937); W. N. Howell, R. Robertson, J. Chem. Soc. 1937, 293; G. Caporale, Farmaco Ed. Sci. 13, 784 (1958); V. K. Ahluwalia et al., Indian J. Chem. 7, 831 (1969). Use in photochemotherapy of psoriasis: H. Hönigsmann et al., Br. J. Dermatol. 101, 369 (1979). Mutagenicity studies: B. R. Scott et al., Mutat. Res. 39, 29 (1976); M. J. Ashwood-Smith et al., Nature 285, 407 (1980). Phototoxicity study: A. Kornhauser et al., Science 217, 733 (1982).

Methoxsalen CAS Registry Number: 298-81-7 花椒毒素; 8-甲氧基补骨脂素

CAS Name: 9-Methoxy-7H-furo[3,2-g][1]benzopyran-7-one
Additional Names: 6-hydroxy-7-methoxy-5-benzofuranacrylic acid d-lactone; 9-methoxypsoralen; 8-methoxy-4',5':6,7-furocoumarin; 8-methoxy[fu...
Literature References: Naturally occurring analog of psoralen, q.v., found in spp. of Leguminosae, Umbelliferae, and Rutaceae. Isolation: Priess, Ber. Dtsch. Pharm. Ges. 21, 227 (1911); Thoms, Ber. 44, 3325 (1911); 45, 3705 (1912); Jois et al., J. Indian Chem. Soc. 10, 41 (1933); Späth et al., Ber. 73, 1361 (1933); Schonberg, Sina, Nature 160, 468 (1947); 161, 481 (1948); J. Am. Chem. Soc. 72, 4826 (1950). Synthesis: Späth, Pailer, Ber. 69, 767 (1936); Lagercrantz, Acta Chem. Scand. 10, 647 (1956); Stanley, Vannier, US 2889337 (1959 to USDA); P. Nore, E. Honkanen, J. Heterocycl. Chem. 17, 985 (1980). Use in treatment of psoriasis and mycosis fungoides: J. A. Parrish et al., Int. J. Dermatol. 19, 379 (1980). Acute toxicity data: Hakim et al., J. Pharmacol. Exp. Ther. 131, 394 (1961). Phototoxicity study: A. Kornhauser et al., Science 217, 733 (1982). Comprehensive description: M. A. Loutfy, M. A. Hassan, Anal. Profiles Drug Subs. 9, 427-454 (1980). Review of use in photochemotherapy: T. F. Anderson, J. J. Voorhees, Annu. Rev. Pharmacol. Toxicol. 20, 235-258 (1980); Acta Derm. Venereol. Suppl. 106, 9-42 (1982).

Urethan CAS Registry Number: 51-79-6 氨基甲酸乙酯

CAS Name: Carbamic acid ethyl ester
Additional Names: ethyl carbamate; urethane; ethyl urethan
Percent Composition: C 40.44%, H 7.92%, N 15.72%, O 35.92%
Literature References: Naturally occurring contaminant in fermented foods, particularly wine, stone-fruit brandies, and bread. Prepd by heating urea with alcohol under pressure; by warming urea nitrate with alcohol and sodium nitrite. Toxicity data: K. J. Franklin, J. Pharmacol. Exp. Ther. 42, 1 (1931). Review of carcinogenic action and metabolism: S. S. Mirvish in Adv. Cancer Res. 11, 1-42 (1968); of mutagenicity, metabolism and interactions with DNA: R. E. Sotomayor, T. F. X. Collins, Toxicol. Ind. Health 6, 71-108 (1990); of physiological effects in animals: K. J. Field, C. M. Lang, Lab. Animals 22, 255-262 (1988). Review of analysis, occurrence and formation in foodstuffs: R. Battaglia et al., Food Addit. Contam. 7, 477-496 (1990); B. Zimmerli, J. Schlatter, Mutat. Res. 259, 325-350 (1991).

Ectoine CAS Registry Number: 96702-03-3 四氢嘧啶(依克多因)

CAS Name: (4S)-1,4,5,6-Tetrahydro-2-methyl-4-pyrimidinecarboxylic acid
Additional Names: ectoin
Trademarks: RonaCare Ectoin (Merck KGaA)
Percent Composition: C 50.69%, H 7.09%, N 19.71%, ...
Literature References: Naturally occurring cyclic amino acid. Organic osmolyte; synthesized by microorganisms to maintain osmotic equilibrium in saline environments and to protect enzymes and whole cells from denaturation. Isoln from the halophilic, phototrophic bacterium, Ectothiorhodospira halochloris, and characterization as a compatible solute: E. A. Galinski et al., Eur. J. Biochem. 149, 135 (1985). Biosynthesis: P. Peters et al., FEMS Microbiol. Lett. 71, 157 (1990). Calorimetric analysis of biosynthesis efficiency: T. Maskow, W. Babel, Biochim. Biophys. Acta 1527, 4 (2001). Chromatographic determn: V. Riis et al., Anal. Bioanal. Chem. 377, 203 (2003). Osmoprotection in E. coli: M. Jebbar et al., J. Bacteriol. 174, 5027 (1992). Mechanism of osmoprotection study: idem et al., ibid. 187, 1293 (2005). Enzyme stabilization study: K. Lippert, E. A. Galinski, Appl. Microbiol. Biotechnol. 37, 61 (1992). In vitro prevention of UVA-induced skin damage: J. Buenger, H. Driller, Skin Pharmacol. Physiol. 17, 232 (2004). Inhibition of b-amyloid peptide aggregation and neurotoxicity: M. Kanapathipillai et al., FEBS Lett. 579, 4775 (2005).