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

Aloxiprin CAS Registry Number: 9014-67-9 阿洛普令

CAS Name: 2-(Acetyloxy)benzoic acid polymer with aluminum oxide
Additional Names: polyoxyaluminum acetylsalicylate
Trademarks: Lyman (Drossapharm); Palaprin (Nicholas); Rumatral (Nicholas)
Literature References: A polymeric condensation product of aluminum oxide and aspirin. Approx formula, Al3O2[C6H4(OOCCH3)COO]5. Prepd from aluminum isopropoxide and aspirin: Cummings et al., J. Pharm. Pharmacol. 15, 56 (1963).

Polybenzarsol CAS Registry Number: 54531-52-1 聚苯胂酸

CAS Name: (4-Hydroxyphenyl)arsonic acid polymer with formaldehyde
Trademarks: Benzodol (Pitman-Moore)
Literature References: A polymeric mixture obtained by adding formaldehyde to p-hydroxybenzenearsonic acid. Prepn: H. E. Faith, J. Am. Chem. Soc. 72, 837 (1950). Toxicity studies: W. R. Jones et al., Antibiot. Chemother. 8, 400 (1958).

Laminaran CAS Registry Number: 9008-22-4 昆布多糖

Additional Names: Laminarin
Literature References: A polysaccharide found in brown seaweed and occurring principally in the Laminaria spp. Linear polymer composed of b-(1®3)-linked glucose residues; may contain small amounts of b-(1®6) linkages as interresidue linkages or as branch points and 2-3% D-mannitol as end groups. Two forms of laminaran are recognized; they are referred to as soluble and insoluble laminaran: Percival, Ross, J. Chem. Soc. 1951, 720. Structure: Peat et al., ibid. 1958, 724, 729; 1960, 175; Goldstein et al., Chem. Ind. (London) 1959, 124; Annan et al., ibid. 1962, 984; Annan et al., J. Chem. Soc. 1965, 885; Maeda, Nisizawa, Carbohydr. Res. 7, 97 (1968). Structure of soluble laminaran from Eisenia bicyclis: T. Usui et al., Agric. Biol. Chem. 43, 603 (1979). NMR studies of laminaran: D. Gagnaire, Org. Magn. Reson. 11, 344 (1978); H. Friebolin et al., ibid. 12, 216 (1979). Review: W. A. P. Black, E. T. Dewar in Industrial Gums, R. L. Whistler, Ed. (Academic Press, New York, 2nd ed., 1973) pp 137-145.

m-Tyrosine CAS Registry Number: 587-33-7 L-间酪氨酸

CAS Name: 3-Hydroxy-L-phenylalanine
Additional Names: a-amino-3-hydroxyhydrocinnamic acid; metatyrosine
Percent Composition: C 59.66%, H 6.12%, N 7.73%, O 26.49%
Literature References: A possible precursor of catecholamines: Sourkes et al., Nature 189, 577 (1961). An intermediate in an alternate pathway for the biosynthesis of catecholamines, where with the existing hydroxylating enzymes m-hydroxylation of phenylalanine to m-tyrosine occurs before p-hydroxylation (forming dopa) and is followed by subsequent decarboxylation to dopamine. Formation in vitro of dopa from L-m-tyrosine: Tong et al., Biochem. Biophys. Res. Commun. 43, 819 (1971); in vivo: Hollunger, Persson, Acta Pharmacol. Toxicol. 34, 391 (1974). Biosynthesis and metabolism studies: D'Iorio et al., Adv. Neurol. 5, 265 (1974). Has also been isolated from a plant source, Euphorbia myrsinites L. Euphorbiaceae: Mothes et al., Z. Naturforsch. 19b, 1161 (1964). m-Tyrosine has the ability to cross the blood-brain barrier and is decarboxylated to m-tyramine which stimulates dopamine receptors, presumably accounting for the demonstrated pharmacological effects of m-tyrosine. Pharmacological studies: Carlsson, Lindqvist, Eur. J. Pharmacol. 2, 187 (1967); Rubenson, J. Pharm. Pharmacol. 23, 228, 412 (1971); Sandler et al., Nature 229, 414 (1971); Ungerstedt et al., Eur. J. Pharmacol. 21, 230 (1973). Crystal and molecular structure: Byrkjedal et al., Acta Chem. Scand. 28B, 750 (1974).

[S-(all-E)]-3-(1,3,5,7,9-Dodecapentaenyloxy)-1,2-propanediol CAS Registry Number: 91423-46-0 (2S)-3-[(1E,3E,5E,7E,9E)-十二碳-1,3,5,7,9-五烯氧基]丙烷-1,2-二醇

Additional Names: Fecapentaene 12
Percent Composition: C 71.97%, H 8.86%, O 19.17%
Literature References: A potent mutagen detected in human feces: W. R. Bruce et al., Cold Spring Harbor Conf. Cell Proliferation 3, 1641 (1977). Isoln and characterization: T. D. Wilkins et al., Am. J. Clin. Nutr. 33, 2513 (1980). Structure: N. Hirai et al., J. Am. Chem. Soc. 104, 6149 (1982). Implicated in human colon cancer: Chem. Eng. News 60, 22 (Sept. 27, 1982); T. H. Maugh, Science 218, 363 (1982).

Acetoin CAS Registry Number: 513-86-0 3-羟基-2-丁酮

CAS Name: 3-Hydroxy-2-butanone
Additional Names: 2,3-butanolone; acetyl methyl carbinol; dimethylketol; g-hydroxy-b-oxobutane
Percent Composition: C 54.53%, H 9.15%, O 36.32%
Literature References: A product of fermentation, also in cream ripened for churning. Obtained by the action of sorbose bacterium or Mycoderma aceti on 2,3-butanediol or by the action of fungi, such as Aspergillus, Penicillium, Mycoderma on sugar cane juice: Browne, J. Am. Chem. Soc. 28, 467 (1906). By action of yeast on diacetyl: Nagelschmidt, Biochem. Z. 186, 317 (1927). From diacetyl by partial reduction with Zn and acid: Diels, Stephan, Ber. 40, 4338 (1907). Fermentation process: Vergnaud, US 2529061 (1950 to Usines de Melle).

Prostacyclin CAS Registry Number: 35121-78-9 依前列醇

CAS Name: (5Z,9a,11a,13E,15S)-6,9-Epoxy-11,15-dihydroxyprosta-5,13-dien-1-oic acid
Additional Names: (5Z)-9-deoxy-6,9a-epoxy-D5-PGF1a; epoprostenol; prostaglandin I2; prostaglandin X; PGI2; PGX...
Literature References: A prostaglandin produced by enzymatic transformation of prostaglandin endoperoxides (PGG2, PGH2), which dilates blood vessels and is approximately 30 times more potent than prostaglandin E1, q.v., in inhibiting platelet aggregation. Evidence for its occurrence during biosynthetic conversion of arachidonic acid by rat stomach homogenates: C. Pace-Asciak, L. S. Wolfe, Biochemistry 10, 3657 (1971). Isoln from microsomes of pig and rabbit aorta by J. R. Vane and co-workers: S. Moncada et al., Nature 263, 663 (1976). Prepn: S. Moncada, N. Whittaker, DE 2720999; S. Moncada, US 4539333 (1977, 1985 both to Wellcome Found.). PGI2 is also synthesized in bovine coronary arteries as well as human arteries and veins: eidem, Lancet 1, 18 (1977); G. J. Dusting et al., Prostaglandins 13, 3 (1977); by cultured human and bovine endothelial cells: B. B. Weksler et al., Proc. Natl. Acad. Sci. USA 74, 3922 (1977); by pig aortic endothelial cells: D. E. MacIntyre et al., Nature 271, 549 (1978). It has been suggested that endoperoxides released by platelets can be converted to PGI2 by vascular tissue and that a balance between formation of PGI2 and release of thromboxane A2, q.v., which induces platelet aggregation, controls the formation of thrombi in blood vessels. It has also been postulated that PGI2 acts to stimulate platelet adenylate cyclase and to prevent the action of thrombi on phospholipid breakdown as well as platelet aggregation. Structure: R. A. Johnson et al., Prostaglandins 12, 915 (1976). Synthesis: E. J. Corey et al., J. Am. Chem. Soc. 99, 3006 (1977); of sodium salt and stereochemistry: R. A. Johnson et al., ibid. 4182. Additional syntheses: I. Tomoskozi et al., Tetrahedron Lett. 1977, 2627; N. Whittaker, ibid. 2805; K. Nicolaou, Chem. Commun. 1977, 630. Synthesis of the 5E-isomer: E. J. Corey et al., Tetrahedron Lett. 1977, 3529. Chemical stability in aq solns: M. J. Cho, M. A. Allen, Prostaglandins 15, 943 (1978). Biosynthetic study: V. Tomasi et al., Nature 273, 670 (1978). Biological properties: R. J. Gryglewski et al., Prostaglandins 12, 685 (1976). Preliminary clinical study: A. E. S. Gimson et al., Lancet 1, 173 (1980). Antimetastatic effects: K. V. Honn et al., Science 212, 1270 (1981); eidem, ibid. 217 542 (1982). Preliminary study of effect of PGX infusion in patients with acute myocardial infarction: O. Edhag et al., N. Engl. J. Med. 308, 1032 (1983). Review of biological properties: S. Moncada, J. R. Vane, Clin. Sci. 61, 369-372 (1981); of therapeutic potential: eidem, Adv. Pharmacol. Ther. 4, 215-233 (1982); of physiological role: J. R. Vane et al., Int. Rev. Exp. Pathol. 23, 161-207 (1982). General reviews: S. Moncada, J. R. Vane, Fed. Proc. 38, 66-71 (1979); J. C. McGiff, Annu. Rev. Pharmacol. Toxicol. 21, 479-509 (1981); S. Moncada et al., Adv. Pharmacol. Ther. 6, 39-47 (1982). Books: Prostacyclin, J. R. Vane, S. Bergstrom, Eds. (Raven Press, New York, 1979) 453 pp; Prostaglandins in Cardiovascular and Renal Function, A. Scriabine et al., Eds. (Spectrum Publications, New York, 1980) 498 pp.

Ficin CAS Registry Number: 9001-33-6 无花果蛋白酶,来源于无花果树乳胶

Additional Names: Ficus proteinase; Ficus protease
Trademarks: Debricin (J J); Higueroxyl Delabarre
Literature References: A proteolytic enzyme of est. mol wt 23,800-25,500 which requires a free sulfhydryl group for activity and as such is a member of a group which includes papain and bromelain, q.q.v. Occurs in the latex of tropical trees of the genus Ficus subgenus Pharmacosyce, Moraceae (Oje trees). The commercial product is a concentrate prepd by filtering and drying the latex of Ficus glabrata H. B. K., Moraceae. First crystallized from fresh fig latex: Walti, J. Am. Chem. Soc. 60, 493 (1938). Characterization: Cohen, Nature 182, 659 (1958); Englund et al., Biochemistry 7, 163 (1968). Purification: Gibian, Bratfisch, US 2950227 (1960 to Schering AG). Amino acid composition: Wong, Liener, Biochem. Biophys. Res. Commun. 17, 470 (1964); Metrione et al., Arch. Biochem. Biophys. 122, 137 (1967); Husain, Lowe, Biochem. J. 117, 333 (1970). Pharmacodynamics: H. Heisto, M. K. Fagerhol, Transfusion 19, 545 (1979); A. Perkash et al., ibid. 20, 301 (1980). Toxicology: H. Molitor et al., J. Pharmacol. Exp. Ther. 71, 20 (1941). Reviews: Liener, Friedenson, Methods Enzymol. 19, 260-273 (1970); Glazer, Smith, The Enzymes vol. III, P. D. Boyer, Ed. (Academic Press, New York, 3rd ed., 1971) pp 538-542.

Keratinase CAS Registry Number: 9025-41-6

Additional Names: M-Zyme
Literature References: A proteolytic enzyme, commercially produced by a strain of Streptomyces fradiae: Nickerson, Noval, US 2988487 (1961 to Rutgers Res. and Educ. Found.). Can convert about 50% of the dry wt of wool into a water-sol form, permitting hair separation from hides. The amount of enzyme needed to dehair hides is not enough to cause much digestion of the hair itself, which is recovered and used in felt making. The enzyme attacks at the base of the hair shaft, which is particularly sensitive to the action of keratinase.

Canadine CAS Registry Number: 522-97-4 L-四氢小檗碱

CAS Name: 5,8,13,13a-Tetrahydro-9,10-dimethoxy-6H-benzo[g]-1,3-benzodioxolo[5,6-a]quinolizine
Additional Names: 9,10-dimethoxy-2,3-(methylenedioxy)berbine; 5,6,13,13a-tetrahydro-9,10-dimethoxy-...
Literature References: A protoberberine alkaloid from Corydalis cava (L.), Schweigg Korte (C. tuberosa DC.), Fumariaceae: Späth, Julian, Ber. 64, 1131 (1931). Prepn by reduction of berberine: Bersch, Seufert, ibid. 70, 1121 (1937); Awe, Hertel, Arch. Pharm. 288, 516 (1955); Russell, J. Am. Chem. Soc. 78, 3115 (1956). Configuration: Corrodi, Hardegger, Helv. Chim. Acta 39, 889 (1956). Other syntheses: Kametani et al., J. Chem. Soc. C 1969, 2036; 1971, 2709; M. Cushman, F. W. Dekon, J. Org. Chem. 44, 407 (1979); K. Iwasa et al., ibid. 46, 4744 (1981); N. S. Narasimhan et al., Tetrahedron Lett. 22, 2797 (1981). Pharmacology: F. Sadritdinov, M. B. Sultanov, C.A. 66, 74714v (1967). Review: R. H. F. Manske, H. L. Holmes, The Alkaloids vol. 4 (Academic Press, New York, 1954) pp 91-92.