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

Showdomycin CAS Registry Number: 16755-07-0 3-beta-D-呋喃核糖基吡咯-2,5-二酮

CAS Name: 3-b-D-Ribofuranosyl-1H-pyrrole-2,5-dione
Additional Names: 2-b-D-ribofuranosylmaleimide
Percent Composition: C 47.16%, H 4.84%, N 6.11%, O 41.89%
Literature References: Nucleoside antibiotic isolated from Streptomyces showdoensis: Nishimura et al., J. Antibiot. 17A, 148 (1964); Nishimura, FR M2751 corresp to US 3316149 (1964, 1967, both to Shionogi). Structure: Nakagawa et al., Tetrahedron Lett. 1967, 4105; Darnall et al., Proc. Natl. Acad. Sci. USA 57, 548 (1967). Synthesis: Kalvoda et al., Tetrahedron Lett. 1970, 2297; Trummlitz, Moffatt, J. Org. Chem. 38, 1841 (1973); T. Sato et al., Tetrahedron Lett. 1978, 1829; J. G. Buchanan et al., J. Chem. Soc. Perkin Trans. 1 1979, 225; T. Inoue, I. Kuwajima, Chem. Commun. 1980, 251; A. P. Kozikowski, A. Ames, J. Am. Chem. Soc. 103, 3923 (1981); Y. Araki et al., Tetrahedron Lett. 29, 351 (1988). Exhibits antitumor activity: Shinzo et al., J. Antibiot. 17A, 234 (1964). Review: D. W. Visser, S. Roy-Burman in Antibiotics vol. 5(pt. 2), F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 363-371.

Mizoribine CAS Registry Number: 50924-49-7 咪唑立宾

CAS Name: 5-Hydroxy-1-b-D-ribofuranosyl-1H-imidazole-4-carboxamide
Additional Names: 4-carbamoyl-1-b-D-ribofuranosylimidazolium-5-olateTrademarks: Bredinin (Toyo Jozo)
Percent Composition: C...
Literature References: Nucleoside antibiotic produced by Eupenicillium brefedianum with cytotoxic and immunosuppressive activity. Isoln: K. Mizuno et al., BE 799805; eidem, US 3888843 (1973, 1975 to Toyo Jozo); eidem, J. Antibiot. 27, 775 (1974). Synthesis: M. Hayashi et al., Chem. Pharm. Bull. 23, 245 (1975); K. Fukukuwa et al., ibid. 32, 1644 (1984). Prepn of the aglycone: T. Atsumi et al., JP Kokai 76 88965 (1976 to Sumitomo), C.A. 86, 106582g (1977). HPLC determn in human serum: K. Takada et al., J. Chromatogr. 222, 156 (1981). Anti-arthritic activity: H. Iwata et al., Experientia 33, 502 (1977). Cytotoxic effect and comparison with aglycone: K. Sakaguchi et al., J. Antibiot. 28, 798 (1975). Antitumor spectrum of aglycone: N. Yoshida et al., Cancer Res. 43, 5851 (1983). Pharmacokinetics: K. Takada, Eur. J. Pharmacol. 24, 457 (1983). Clinical trials in renal transplantation: T. Inou et al., Transplant. Proc. 12, 526 (1980); eidem, ibid. 13, 315 (1981); A. Tajima et al., Transplantation 38, 116 (1984).

Blasticidin S CAS Registry Number: 2079-00-7 布拉叶斯

CAS Name: 4-[[3-Amino-5-[(aminoiminomethyl)methylamino]-1-oxopentyl]amino]-1-(4-amino-2-oxo-1(2H)-pyrimidinyl)-1,2,3,4-tetradeoxy-b-D-erythro-hex-2-enopyranuronic acid
Additional Names: 4-[3-am...
Literature References: Nucleoside antibiotic produced by Streptomyces griseochromogenes: Isoln and antimicrobial activity: Takeuchi et al., J. Antibiot. 11A, 1 (1958); Sumiki, Umezawa, JP 60 16449 (1960 to Japan Antibiot. Res. Assoc.), C.A. 55, 21474e (1961). Structure: Otake et al., Agric. Biol. Chem. 30, 132 (1966); Fox, Watanabe, Tetrahedron Lett. 1966, 897. Abs config: Yonehara et al., ibid. 1966, 3785. Synthesis of the unsaturated carbohydrate: Goody et al., ibid. 1970, 293; of the cytosinine moiety: Fox, Watanabe, Pure Appl. Chem. 28, 475 (1971); Kondo et al., Tetrahedron Lett. 1972, 1881; eidem, Tetrahedron 29, 1801 (1973). Crystal and molecular structure: V. Swaminathan et al., Biochim. Biophys. Acta 655, 335 (1981).

Psicofuranine CAS Registry Number: 1874-54-0 阿洛酮糖腺苷

CAS Name: 9-b-D-Psicofuranosyl-9H-purin-6-amine
Additional Names: 9b-D-psicofuranosyladenine; 6-amino-9-D-psicofuranosylpurine; angustmycin CPercent Composition: C 44.44%, H 5.09%, N 23.56%, O ...
Literature References: Nucleoside antibiotic produced by Streptomyces hygroscopicus var. decoyicus: Eble et al., Antibiot. Chemother. 9, 419 (1959); Yüntsen, J. Antibiot. 11A, 244 (1958); Eble, Lewis, US 3020274 (1962 to Upjohn). Antibacterial and antitumor activity: N. Tanaka et al., J. Antibiot. 14A, 98 (1961). Structure: Schroeder, Hoeksema, J. Am. Chem. Soc. 81, 1767 (1959); Garrett, ibid. 82, 827 (1960). Synthesis: Farkas, Sorm, Collect. Czech. Chem. Commun. 28, 882 (1963); L. A. Aleksandrova, F. W. Lichtenthaler, Nucleic Acids Symp. Ser. 9, 263 (1981). Biosynthesis: Sugimori, Suhadolnik, J. Am. Chem. Soc. 87, 1136 (1965). Inhibits the conversion of xanthosine-5¢-phosphate to guanosine-5¢-phosphate: Slechta, Biochem. Pharmacol. 5, 96 (1960).

a -Ribazole CAS Registry Number: 132-13-8 (2S,3R,4S,5R)-2-(5,6-二甲基苯并咪唑-1-基)-5-(羟基甲基)四氢呋喃-3,4-二醇

CAS Name: 5,6-Dimethyl-1-a-D-ribofuranosyl-1H-benzimidazole
Percent Composition: C 60.42%, H 6.52%, N 10.07%, O 23.00%
Literature References: Nucleoside moiety of vitamin B12, q.v. Isoln by acid hydrolysis of vitamin B12: N. G. Brink et al., J. Am. Chem. Soc. 72, 1866 (1950); N. G. Brink, K. Folkers, ibid. 74, 2856 (1952). Syntheses of a- and b-anomers: F. W. Holly et al., ibid. 4521; R. S. Wright et al., ibid. 80, 2004 (1958); J. D. Stevens et al., J. Org. Chem. 33, 1806 (1968). Biosynthetic study: J. Hörig, P. Renz, FEBS Lett. 80, 337 (1977). Spectroscopic characterization: K. L. Brown et al., Inorg. Chem. 23, 1463 (1984).

Abacavir CAS Registry Number: 136470-78-5 阿巴卡韦

CAS Name: (1S,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol
Additional Names: (-)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanolPerc...
Literature References: Nucleoside reverse transcriptase inhibitor (NRTI). Prepn: S. M. Daluge, EP 349242 (1990 to Wellcome Found.); idem, US 5034394 (1991 to Burroughs Wellcome). Asymmetric synthesis: M. T. Crimmins, B. W. King, J. Org. Chem. 61, 4192 (1996). Pharmacology and biological profile: S. M. Daluge et al., Antimicrob. Agents Chemother. 41, 1082 (1997). Review of antiviral activity and clinical evaluations: R. H. Foster, D. Faulds, Drugs 55, 729-736 (1998). Clinical trial of triple nucleoside regimen in HIV patients: S. Staszewski et al., J. Am. Med. Assoc. 285, 1155 (2001).

Diclazuril CAS Registry Number: 101831-37-2 地克珠利

CAS Name: 2,6-Dichloro-a-(4-chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)benzeneacetonitrile
Additional Names: (p-chlorophenyl)[2,6-dichloro-4-(4,5-dihydro-3,5-dioxo-as-triazin...
Literature References: Nucleotide analog with broad-spectrum anticoccidial activity. Prepn: G. M. Boeckx et al., EP 170316; eidem, US 4631278 (both 1986 to Janssen). Mechanism of action studies: L. Maes et al., J. Parasitol. 74, 931 (1988); A. Verheyen et al., ibid. 939. Efficacy against Eimeria species in turkeys: O. Vanparijs et al., Avian Dis. 33, 479 (1989); in chickens: O. Vanparijs et al., Poult. Sci. 69, 60 (1990). Preliminary evaluation in coccidial enteritis in AIDS patients: K. Kayembe et al., Lancet 1, 1397 (1989).

Bipiperidyl Mustard CAS Registry Number: 6802-93-3 1,1'-二(2-氯乙基)-4,4'-联哌啶

CAS Name: 1,1'-Bis(2-chloroethyl)-4,4'-bipiperidine
Additional Names: BPM
Percent Composition: C 57.33%, H 8.94%, Cl 24.18%, N 9.55%
Literature References: Obesifying agent causing rapid lipid deposition in mice: Rutman et al., Science 153, 1000 (1966). Activity shown only by the active form, prepd by neutralizing the conjugate acid form and generating a bicyclic ammonium deriv at pH 10. Metabolic studies: eidem, Trans. N.Y. Acad. Sci. 30, 244 (1967). Research use for obesity-producing brain lesions: H.-R. Berthoud, T. L. Powley, Am. J. Physiol. 248, R46 (1985); A. C. Scallet, J. W. Olney, Brain Res. 374, 380 (1986). Toxicity study: E. W. Schafer, Jr. et al., Ecotoxicol. Environ. Saf. 6, 149 (1982).

Succinic Acid CAS Registry Number: 110-15-6 琥珀酸; 丁二酸

CAS Name: Butanedioic acid
Additional Names: amber acid; ethylenesuccinic acid; Bernsteinsäure (German)
Trademarks: Asuccin
Percent Composition: C 40.68%, H 5.12%, O 54.19%
Literature References: Observed by Agricola in 1546, in the distillate from amber. Occurs in fossils, fungi, lichens, etc. Prepn from acetic acid: Coffman et al., J. Am. Chem. Soc. 80, 2864 (1958). Manuf: Crosby, Braunwarth, US 2862028 (1958 to Pure Oil); Chafetz, Patterson, US 2978473 (1961 to Texaco). Toxicity study: H. F. Smyth et al., Arch. Ind. Hyg. Occup. Med. 4, 119 (1951).

Opianic Acid CAS Registry Number: 519-05-1 2-羧基-3,4-二甲氧基苯甲醛

CAS Name: 6-Formyl-2,3-dimethoxybenzoic acid
Additional Names: 5,6-dimethoxyphthalaldehydic acid
Percent Composition: C 57.14%, H 4.80%, O 38.06%
Literature References: Obtained (together with cotarnine) by heating narcotine with dil HNO3. Prepn: Wilson et al., J. Org. Chem. 16, 792 (1951); Blair, J. Chem. Soc. 1955, 708. NMR studies: Buu-Hoi et al., Bull. Soc. Chim. Fr. 1970, 137.