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

Equilin CAS Registry Number: 474-86-2 马烯雌酮

CAS Name: 3-Hydroxyestra-1,3,5(10),7-tetraen-17-one
Additional Names: 1,3,5,7-estratetraen-3-ol-17-one
Percent Composition: C 80.56%, H 7.51%, O 11.92%
Literature References: Steroidal hormone isolated from urine of pregnant mares: Girard et al., Compt. Rend. 195, 981 (1932); Cartland, Meyer, J. Biol. Chem. 112, 9 (1935/6). Structure: Serini, Logemann, Ber. 71, 186 (1938); Pearlman, Wintersteiner, J. Biol. Chem. 130, 35 (1939). Separation from estrone: Serini, Logemann, US 2221340 (1941 to Schering). Synthesis: Zderic et al., J. Am. Chem. Soc. 80, 2596 (1958); Bagli et al., Tetrahedron Lett. 1964, 387; Stein et al., ibid. 1966, 5015; eidem, Tetrahedron 26, 1917 (1970). Prepn from testosterone by bacterial fermentation: Bowers et al., US 3067212 (1962 to Syntex). Prepn by conversion of equilenin: Bailey et al., Chem. Commun. 1967, 1253; Marshall, Deghenghi, Can. J. Chem. 47, 3127 (1969). Component of Conjugated Estrogenic Hormones, q.v. Review of synthetic studies: Taub, "Naturally Occurring Aromatic Steroids" in The Total Synthesis of Natural Products vol. 2, J. ApSimon, Ed. (John Wiley Sons, New York, 1973) pp 664-670.

Somatoliberin CAS Registry Number: 83930-13-6 生长释素

CAS Name: Growth hormone-releasing factor
Additional Names: GH-RF; GH-RH; GRF; growth hormone-releasing hormone; hGRF; hpGRF; somatocrinin
Literature References: Stimulatory growth-hormone releasing factor of the hypothalamus that mediates, together with somatostatin, q.v., the neuroregulation of somatotropin secretion. The concept of hypothalamic regulation of growth hormone release was postulated on the basis of physiological and biochemical evidence, cf. A. V. Schally et al., Recent Prog. Horm. Res. 24, 497 (1968); J. B. Martin in Frontiers in Neuroendocrinology, L. Martini, W. F. Ganong, Eds. (Raven Press, New York, 1976) pp 129-168. Demonstration of the existence of a GH-RH: R. Deuben, J. Meites, Endocrinology 74, 408 (1964); A. V. Schally et al., ibid. 82, 271 (1968); E. Dickermann et al., Neuroendocrinology 4, 75 (1969). Isoln of a decapeptide originally believed to be GRF: A. V. Schally et al., Endocrinology 84, 1493 (1969). Review of early literature: eidem, Science 179, 341 (1973). Isoln and characterization of hpGRF, a fully bioactive, 44 amino acid peptide from human pancreatic tumor: R. Guillemin et al., Science 218, 585 (1982); J. Rivier et al., Nature 300, 276 (1982). Cloning and sequence analysis of cDNA for hpGRF precursor: U. Gubler et al., Proc. Natl. Acad. Sci. USA 80, 4311 (1983). Expression-cloning of cDNA for hpGRF: K. E. Mayo et al., Nature 306, 86 (1983). Isoln, primary structure and synthesis of native human hypothalamic GRF (hGRF), identity with hpGRF and comparison with GRF from other species: N. Ling et al., Proc. Natl. Acad. Sci. USA 81, 4302 (1984). Immunohistochemical detection of GRF in brain: B. Bloch et al., ibid. 301, 607 (1983). Potent interaction of glucocorticoids with GRF in vivo: W. B. Wehrenberg et al., Science 221, 556 (1983). Series of articles on clinical pharmacology: Horm. Res. 22, 32-57 (1985). Clinical evaluation in treatment of hypopituitary dwarfism: M. O. Thorner et al., N. Engl. J. Med. 312, 4 (1985). Reviews: R. Guillemin et al., Recent Prog. Horm. Res. 40, 233-299 (1984); W. B. Wehrenberg et al., Annu. Rev. Pharmacol. Toxicol. 25, 463-483 (1985).

Picoxystrobin CAS Registry Number: 117428-22-5 啶氧菌酯

CAS Name: (aE)-a-(Methoxymethylene)-2-[[[6-(trifluoromethyl)-2-pyridinyl]oxy]methyl]benzeneacetic acid methyl ester
Additional Names: methyl (E)-2-[2-[6-(trifluoromethyl)pyridin-2-yloxymethyl]p...
Literature References: Strobilurin fungicide for use in cereal crops. Prepn: J. M. Clough et al., EP 278595; eidem, US 5021581 (1988, 1991 both to ICI). Comprehensive description: J. R. Godwin et al., Brighton Crop Prot. Conf. - Pests Dis. 2000, 533-540; M. Hiemer et al., Gesunde Pflanz. 53, 191-195 (2001).

Pyraclostrobin CAS Registry Number: 175013-18-0 吡唑醚菌酯

CAS Name: [2-[[[1-(4-Chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]phenyl]methoxycarbamic acid methyl ester
Additional Names: methyl N-[2-[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxymethyl]phenyl]-N-met...
Literature References: Strobilurin fungicide for use in seed grass and food crops. Prepn: B. Müller et al., DE 4423612; eidem, US 5869517 (1996, 1999 both to BASF). Comprehensive description: E. Ammermann et al., Brighton Crop Prot. Conf. - Pests Dis. 2000, 541-548. Review of activity and field trials: R. Stierl et al., ibid. 859-864.

Amarogentin CAS Registry Number: 21018-84-8 苦龙胆酯苷

CAS Name: [4aS-(4aa,5b,6a)]-3,3',5-Trihydroxy[1,1'-biphenyl]-2-carboxylic acid 2-ester with 5-ethenyl-6-(b-D-glucopyranosyloxy)-4,4a,5,6-tetrahydro-1H,3H-pyrano[3,4-c]pyran-1-one
Additional Nam...
Literature References: Strongly bitter glucoside. Isoln from Swertia chirata Buch-Ham., Gentianaceae: Korte, Ber. 88, 704 (1955); 89, 2404 (1956); from Swertia japonica Makino: Inouye et al., Chem. Pharm. Bull. 18, 1856 (1970). Occurrence in gentianaceous plants: Inouye, Nakamura, J. Pharm. Soc. Jpn. 91, 755 (1971), C.A. 75, 95431b (1971). Structure: eidem, Tetrahedron Lett. 1968, 4919; eidem, Tetrahedron 27, 1951 (1971).

Pirarubicin CAS Registry Number: 72496-41-4 吡柔比星

CAS Name: (8S,10S)-10-[[3-Amino-2,3,6-trideoxy-4-O-[(2S)-tetrahydro-2H-pyran-2-yl]-a-L-lyxo-hexopyranosyl]oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-5,12-naphthacenedio...
Literature References: Structural analog of doxorubicin, q.v. Prepn of (2¢¢R) and (2¢¢S)-diastereomers: H. Umezawa et al., J. Antibiot. 32, 1082 (1979); idem et al., EP 14853; eidem, US 4303785 (1980, 1981 both to Microbiochem. Res. Found. Japan). Absolute configuration: idem et al., J. Antibiot. 37, 1094 (1984). HPLC determn in biological fluids: Y. Matsushita et al., ibid. 36, 880 (1983). Cellular uptake and inhibition of DNA synthesis: S. Kunimoto et al., ibid. 312 (1983). Mechanism of action study: K.-I. Kiyomiya et al., Int. J. Oncol. 21, 1081 (2002). Clinical pharmacokinetics and toxicity: A. A. Miller, C. G. Schmidt, Cancer Res. 47, 1461 (1987). Overview of clinical experience: H. Majima, K. Ohta, Biomed. Pharmacother. 41, 237-243 (1987). Clinical evaluation in metastatic colon cancer: D. Fallik et al., Ann. Oncol. 14, 856 (2003)

Pregabalin CAS Registry Number: 148553-50-8 普瑞巴林

CAS Name: (3S)-3-(Aminomethyl)-5-methylhexanoic acid
Additional Names: (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid; (S)-(+)-3-isobutyl-g-aminobutyric acidTrademarks: Lyrica (Pfizer)
Perc...
Literature References: Structural analog of g-aminobutyric acid, q.v.; ligand at a2d subunit of voltage-gated calcium channels. Prepn of racemate: R. Andruszkiewicz, R. B. Silverman, Synthesis 1989, 953. Enantioselective synthesis: P. Yuen et al., Bioorg. Med. Chem. Lett. 4, 823 (1994). Manufacturing process: M. S. Hoekstra et al., Org. Process Res. Dev. 1, 26 (1997). HPLC determn in biological fluids: B. L. Windsor, L. L. Radulovic, J. Chromatogr. B 674, 143 (1995). Clinical trial in post-herpetic neuralgia: R. Sabatowski et al., Pain 109, 26 (2004). Overview of mechanism and pharmacology: S. M. Stahl, J. Clin. Psychiatry 65, 596, 1033 (2004). Review of pharmacology and clinical experience: B. A. Lauria-Horner, R. B. Pohl, Expert Opin. Invest. Drugs 12, 663-672 (2003); R. Huckle, Curr. Opin. Invest. Drugs 5, 82-89 (2004).

Pilsicainide CAS Registry Number: 88069-67-4 吡西卡尼

CAS Name: N-(2,6-Dimethylphenyl)tetrahydro-1H-pyrrolizine-7a(5H)-acetamide
Additional Names: tetrahydro-1H-pyrrolizine-7a(5H)-aceto-2',6'-xylidide; N-(2,6-dimethylphenyl)-8-pyrrolizidineacetami...
Literature References: Structural analog of lidocaine, q.v. Prepn: S. Miyano et al., EP 89061; eidem, US 4564624 (1983, 1986 both to Suntory); eidem, J. Med. Chem. 28, 714 (1985). Pharmacology: K. Aisaka et al., Arzneim.-Forsch. 35, 1239 (1985); T. Hidaka et al., ibid. 1381. Clinical evaluation in supraventricular tachycardia: T. Terazawa et al., Am. Heart J. 121, 1437 (1991).

Coumachlor CAS Registry Number: 81-82-3 氯华法林

CAS Name: 3-[1-(4-Chlorophenyl)-3-oxobutyl]-4-hydroxy-2H-1-benzopyran-2-one
Additional Names: 3-(a-acetonyl-p-chlorobenzyl)-4-hydroxycoumarin; 3-(a-p-chlorophenyl-b-acetylethyl)-4-hydroxycoumar...
Literature References: Structural analog of warfarin. Prepn: F. Litvan, W. Stoll, US 2648682 (1953 to J. R. Geigy). Anticoagulant activity: M. Reiff, R. Weismann, Acta Trop. 8, 97 (1951), C.A. 50, 10976d (1956). Review of comparative toxicology: H. Wanntorp, Acta Pharmacol. Toxicol. 16, Suppl. 2, 123 pp (1959).

Tioxidazole CAS Registry Number: 61570-90-9 噻昔达唑

CAS Name: (6-Propoxy-2-benzothiazolyl)carbamic acid methyl ester
Additional Names: methyl 6-propoxy-2-benzothiazolylcarbamateTrademarks: Tiox (Schering-Plough)
Percent Composition: C 54.12%,...
Literature References: Structurally related to benzimidazole anthelmintics. Prepn and anthelmintic activity: M. M. Nafissi-Varchei, BE 840945; US 4006242 (1976, 1977 both to Schering). Physical data, activity against roundworms: E. Panitz et al., Experientia 34, 733 (1978). Anthelmintic effect against gastrointestinal parasites in naturally infected horses: J. H. Drudge et al., Am. J. Vet. Res. 41, 1383 (1980); E. T. Lyons et al., ibid. 42, 1048 (1981).