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

Sulfazecin CAS Registry Number: 77912-79-9 (2S)-2-氨基-5-[[(2R)-2-[[(3R)-3-甲氧基-2-氧代-1-磺基氮杂环丁-3-基]氨基]丙酰]氨基]-5-氧代戊酸

CAS Name: D-g-Glutamyl-N-[(3R)-3-methoxy-2-oxo-1-sulfo-3-azetidinyl]-D-alaninamide
Additional Names: 3-g-D-glutamyl-D-alanylamino-3-methoxyazetidin-2-one-1-sulfonic acid; (3R)-3-(g-D-glutamyl-D...
Literature References: Novel monocyclic b-lactam (monobactam) antibiotic, produced by Pseudomonas acidophila and P. mesoacidophila. Isoln, description of physico-chemical and bacteriostatic properties: A. Imada et al., DE 2855949 corresp to US 4229436 (1979, 1980 both to Takeda); eidem, Nature 289, 590 (1981); M. Asai et al., J. Antibiot. 34, 621 (1981). X-ray crystallographic structure determn: K. Kamiya et al., Acta Crystallogr. B37, 1626 (1981). Prepn of fluorinated sulfazecin analogs: K.Yoshioka et al., J. Org. Chem. 49, 1427 (1984); P. F. Bevilacqua et al., ibid. 1430.

Oxetorone CAS Registry Number: 26020-55-3 奥昔托隆

CAS Name: 3-Benzofuro[3,2-c][1]benzoxepin-6(12H)-ylidene-N,N-dimethyl-1-propanamine
Additional Names: N,N-dimethylbenzofuro[3,2-c][1]benzoxepin-D6(12H),g-propylamine; 6-(3-dimethylaminopropylid...
Literature References: Novel serotonin and histamine antagonist with antimigraine activity. Prepn: F. Binon, M. Descamps, DE 1963205 corresp to US 3651051 (1970, 1972 both to Labaz). Metabolism in vitro: E. Rossi et al., J. Chromatogr. 152, 228 (1978). Use in treatment of migraine: J. J. Dufresne, Praxis 67, 1148 (1978); J. Florence, ibid. 1323; in chronic headache: U. Thoden, Therapiewoche 30, 492 (1980).

Aphidicolin CAS Registry Number: 38966-21-1 阿非科林

CAS Name: (3a,4a,5a,17a)-3,17-Dihydroxy-4-methyl-9,15-cyclo-C,18-dinor-14,15-secoandrostane-4,17-dimethanol
Additional Names: tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-8,11a-methano-11aH-cycl...
Literature References: Novel tetracyclic diterpene antibiotic with antiviral and antimitotic properties, isolated as (+)-form from Cephalosporium aphidicola Petch. Specific inhibitor of DNA a-polymerase. Description and x-ray crystallographic determn of structure: K. M. Brundret et al., Chem. Commun. 1972, 1027. Prepn and antiviral activity: A. Borrow et al., US 3761512 (1973 to ICI). Structure and abs config: W. Dalziel et al., J. Chem. Soc. Perkin Trans. 1 1973, 2841. Total synthesis of (±)-aphidicolin: B. M. Trost et al., J. Am. Chem. Soc. 101, 1328 (1979); J. E. McMurry et al., ibid. 1331; E. J. Corey et al., ibid. 102, 1743 (1980); J. E. McMurry et al., Tetrahedron 37, Suppl. 1, 319 (1981). Antiviral effects in vitro and in vivo: R. A. Bucknall et al., Antimicrob. Agents Chemother. 4, 294 (1973). Antimitotic activity: S. Ikegami et al., Nature 275, 458 (1978). Effects on DNA synthesis in mouse sarcoma: S. Seki et al., Biochim. Biophys. Acta 610, 413 (1980). Enzymatic determn method: G. Pedrali-Noy et al., J. Biochem. Biophys. Methods 4, 113 (1981). Induction of differentiation of human myeloid leukemia cells: J. Griffin et al., Exp. Hematol. 10, 774 (1982). Effects on cell proliferation: G. Iliakis et al., Int. J. Radiat. Biol. 42, 417 (1982); on g-irradiated human fibroblasts: P. J. Smith, M. C. Paterson, Biochim. Biophys. Acta 739, 17 (1983).

Olah's Reagent CAS Registry Number: 62778-11-4 吡啶氢氟酸盐

CAS Name: Hydrofluoric acid homopolymer compd with pyridine
Additional Names: pyridinium poly(hydrogen fluoride); PPHF
Literature References: Nucleophilic fluorinating agent; acts as a stabilized, less volatile form of hydrogen fluoride, q.v. Consists of approx 30% pyridine and 70% hydrogen fluoride (w/w) in equilibrium with a small amount of free hydrogen fluoride. Use in fluorination of steroids: C. G. Bergstrom et al., J. Org. Chem. 28, 2633 (1963). Prepn and use as an organic fluorinating reagent: G. A. Olah et al., Synthesis 1973, 779; idem et al., J. Org. Chem. 44, 3872 (1979). Peptide deprotection: S. Matsuura et al., J. Chem. Soc. Chem. Commun. 1976, 451. Review of use in organic synthesis: G. A. Olah et al., J. Fluorine Chem. 33, 377-396 (1986).

Aminoguanidine CAS Registry Number: 79-17-4 氨基胍盐酸盐

CAS Name: Hydrazinecarboximidamide
Additional Names: guanylhydrazine; pimagedine
Percent Composition: C 16.21%, H 8.16%, N 75.62%
Literature References: Nucleophilic hydrazine; inhibits the formation of advanced glycosylation end products (AGEs) that have been implicated in the etiology of diabetic complications. Prepn: J. Thiele, Ann. 270, 1 (1892); G. B. L. Smith, E. Anzelmi, J. Am. Chem. Soc. 57, 2730 (1935). Review of chemistry of aminoguanidine and related compounds: E. Lieber, G. B. L. Smith, Chem. Rev. 25, 213-271 (1939); of preparative methods: F. Kurzer, L. E. A. Godfrey, Chem. Ind. (London) 1962, 1584-1595. Prevention of glucose-derived aortic collagen cross-linking in diabetic rats: M. Brownlee et al., Science 232, 1629 (1986). Mechanism of action study: D. Edelstein, M. Brownlee, Diabetes 41, 26 (1992). Review of therapeutic potential: B. H. R. Wolffenbuttel, M. S. P. Huijberts, Neth. J. Med. 42, 205-208 (1993).

Ganciclovir CAS Registry Number: 82410-32-0 更昔洛韦

CAS Name: 2-Amino-1,9-dihydro-9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]-6H-purin-6-one
Additional Names: 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine; 2'-nor-2'-deoxyguanosine; DHPG; 2'NDGPer...
Literature References: Nucleoside analog structurally related to acyclovir, q.v. Prepn: J. P. Verheyden, J. C. Martin, US 4355032 (1982 to Syntex); K. K. Ogilvie et al., Can. J. Chem. 60, 3005 (1982); W. T. Ashton et al., Biochem. Biophys. Res. Commun. 108, 1716 (1982); J. C. Martin et al., J. Med. Chem. 26, 759 (1983). Antiviral spectrum in vitro: K. O. Smith et al., Antimicrob. Agents Chemother. 22, 55 (1982). Mode of action study: Y.-C. Cheng et al., Proc. Natl. Acad. Sci. USA 80, 2767 (1983). Clinical treatment of cytomegalovirus infection in immunodeficient patients: S. H. Koretz et al., N. Engl. J. Med. 314, 801 (1986). Symposium on pharmacology and clinical efficacy vs cytomegalovirus: Rev. Infect. Dis. 10, Suppl. 3, S457-S572 (1988). Review: C. S. Crumpacker, N. Engl. J. Med. 335, 721-729 (1996).

Tiazofurin CAS Registry Number: 60084-10-8 噻唑呋林

CAS Name: 2b-D-Ribofuranosyl-4-thiazolecarboxamide
Additional Names: riboxamide; TCARTrademarks: Tiazole (ICN)
Percent Composition: C 41.53%, H 4.65%, N 10.76%, O 30.74%, S 12.32%
Literature References: Nucleoside analog that inhibits inosine monophosphate dehydrogenase (IMPDH). Prepn: M. Fuertes et al., J. Org. Chem. 41, 4074 (1976); and antiviral activity: P. C. Srivastava et al., J. Med. Chem. 20, 256 (1977). Structure-activity study: G. Gebeyehu et al., ibid. 28, 99 (1985). HPLC determn in plasma: R. W. Klecker, Jr., J. M. Collins, J. Chromatogr. 307, 361 (1984). Clinical pharmacokinetics: D. Raghavan et al., Cancer Chemother. Pharmacol. 16, 160 (1986). Clinical evaluation in leukemia: G. Tricot et al, Int. J. Cell Cloning 8, 161 (1990). Series of articles on pharmacology and clinical experience: Anticancer Res. 16, 3307-3354 (1996).

Cytarabine CAS Registry Number: 147-94-4 阿糖胞苷

CAS Name: 4-Amino-1-b-D-arabinofuranosyl-2(1H)-pyrimidinone
Additional Names: 1-b-D-arabinofuranosylcytosine; Ara-C; b-cytosine arabinoside; aracytidineTrademarks: Alexan (Ebewe); Aracytine (Pf...
Literature References: Nucleoside analog; converted by cellular kinases into the active metabolite, AraCTP. Prepn: J. H. Hunter, US 3116282 (1963 to Upjohn); T. Y. Shen et al., J. Org. Chem. 30, 835 (1965). NMR soln structure of Ara-C within a DNA dodecamer: B. I. Schweitzer et al., Biochemistry 33, 11460 (1994). Crystal structure of complex with human topoisomerase I: J. E. Chrencik et al., J. Biol. Chem. 278, 12461 (2003). Clinical pharmacology and toxicology: R. C. Donehower et al., Cancer Treat. Rep. 70, 1059 (1986). Symposium on clinical pharmacology, pharmacokinetics and efficacy in leukemia: Scand. J. Haematol. 36, Suppl. 44, 1-74 (1986). Review of development of a high dose treatment for acute myeloid leukemia: R. L. Capizzi, Invest. New Drugs 14, 249-256 (1996); of cellular metabolism and mechanism of action: S. Grant, Adv. Cancer Res. 72, 197-233 (1998).

Telbivudine CAS Registry Number: 3424-98-4 替比夫定

CAS Name: 1-(2-Deoxy-b-L-erythro-pentofuranosyl)-5-methyl-2,4(1H,3H)-pyrimidinedione
Additional Names: 1,2'-deoxy-b-L-ribofuranosylthymine; 2'-deoxy-L-thymidine; LdT; L-thymidine
Percent Com...
Literature References: Nucleoside analog; specific inhibitor of hepatitis B virus (HBV) replication. Prepn: J. Smejkal, F. Sorm, Collect. Czech. Chem. Commun. 29, 2809 (1964); A. Holy, ibid. 37, 4072 (1972). Anti-HBV activity: M. L. Bryant et al., Nucleosides Nucleotides Nucleic Acids 20, 597 (2001). In vitro pharmacology: B. Hernandez-Santiago et al., Antimicrob. Agents Chemother. 46, 1728 (2002). Clinical evaluation in hepatitis B: C.-L. Lai et al., Hepatology 40, 719 (2004). Review of mechanism of action and pharmacology: D. N. Standring et al., Antiviral Chem. Chemother. 12, Suppl. 1, 119-129 (2001); of clinical development: S.-H. B. Han, Expert Opin. Invest. Drugs 14, 511-519 (2005). See also Thymidine.

Clevudine CAS Registry Number: 163252-36-6 克拉夫定

CAS Name: 1-(2-Deoxy-2-fluoro-b-L-arabinofuranosyl)-5-methyl-2,4-(1H,3H)-pyrimidinedione
Additional Names: 1-(2-deoxy-2-fluoro-b-L-arabinofuranosyl)thymine; 2'-fluoro-5-methyl-b-L-arabinofurano...
Literature References: Nucleoside analog; specific inhibitor of viral DNA synthesis. Prepn: C. K. Chu et al., WO 9520595; eidem, US 5587362 (1995, 1996 both to Univ. Georgia Res. Found.; Yale Univ.); T. Ma et al., J. Med. Chem. 39, 2835 (1996). Synthesis: M. L. Sznaidman et al., Nucleosides Nucleotides Nucleic Acids 21, 155 (2002). In vitro antiviral activity: C. K. Chu et al., Antimicrob. Agents Chemother. 39, 979 (1995). Pharmacokinetics: J. D. Wright et al., Pharm. Res. 12, 1350 (1995). Mechanism of action study: Y. Chong, C. K. Chu, Bioorg. Med. Chem. Lett. 12, 3459 (2002). Clinical evaluation in chronic hepatitis B: P. Marcellin et al., Hepatology 40, 140 (2004). Review of preclinical pharmacology: C. K. Chu et al. in Therapies for Viral Hepatitis, R. F. Schinazi et al., Eds. (Int. Med. Press, London, 1998) pp 303-312; of development and clinical experience: G. R. Painter et al. in Frontiers in Viral Hepatitis, R. F. Schinazi et al., Eds. (Elsevier, New York, 2003) pp 281-300.