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

Plaunotol CAS Registry Number: 64218-02-6 谱劳诺托

CAS Name: (2Z,6E)-2-[(3E)-4,8-Dimethyl-3,7-nonadienyl]-6-methyl-2,6-octadiene-1,8-diol
Additional Names: (E,Z,E)-7-hydroxymethyl-3,11,15-trimethyl-2,6,10,14-hexadecatetraen-1-olTrademarks: Keln...
Literature References: Acyclic diterpene alcohol isolated from a Thai medicinal plant identified as Croton sublyratus Kurz, Euphorbiaceae. Isoln, synthesis and anti-ulcer activity: H. Mishima et al., JP Kokai 77 62213; eidem, US 4059641 (both 1977 to Sankyo); A. Ogiso et al., Chem. Pharm. Bull. 26, 3117 (1978). Pharmacology: S. Kobayashi et al., Oyo Yakuri 24, 599 (1982).

Adefovir CAS Registry Number: 106941-25-7 阿德福韦

CAS Name: [[2-(6-Amino-9H-purin-9-yl)ethoxy]methyl]phosphonic acid
Additional Names: 9-(2-phosphonylmethoxyethyl)adenine; PMEAPercent Composition: C 35.17%, H 4.43%, N 25.64%, O 23.43%, P 11.34...
Literature References: Acyclic nucleoside phosphonate (ANP) analog. Prepn: A. Holy, I. Rosenberg, EP 206459; eidem, US 4808716 (1986, 1989 both to Ceskoslov. Akad. Ved); eidem, Collect. Czech. Chem. Commun. 52, 2801 (1987); of dipivoxil ester prodrug: J. E. Starrett, Jr. et al., EP 481214 (1992 to Bristol-Myers Squibb); eidem, US 5663159 (1997 to Inst. Org. Chem. Biochem. Acad. Sci. Czech Rep.; Rega). Crystal structure: C. H. Schwalbe et al., J. Chem. Soc. Perkin Trans. 1 1991, 1348. HPLC determn: P. Augustijns et al., J. Liq. Chromatogr. Relat. Technol. 19, 2271 (1996). Clinical pharmacokinetics: K. C. Cundy et al., Antimicrob. Agents Chemother. 39, 2401 (1995). Review of pharmacology and therapeutic potential: L. Naesens et al., Antiviral Chem. Chemother. 8, 1-23 (1997). Clinical trial in HIV infected patients: J. Kahn et al., J. Am. Med. Assoc. 282, 2305 (1999); in hepatitis B virus (HBV): R. J. C. Gilson et al, J. Viral Hepat. 6, 387 (1999). Resistance surveillance in HBV infections: H. Yang et al., Hepatology 36, 464 (2002).

Tenofovir CAS Registry Number: 147127-20-6 泰诺福韦

CAS Name: [[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic acid
Additional Names: (R)-9-(2-phosphonomethoxypropyl)adenine; (R)-PMPAPercent Composition: C 37.64%, H 4.91%, N 24....
Literature References: Acyclic phosphonate nucleotide analog; reverse transcriptase inhibitor. Prepn: I. Rosenberg et al., Collect. Czech. Chem. Commun. 53, 2753 (1988); A. Holy et al., ibid. 60, 1390 (1995); L. M. Schultze et al., Tetrahedron Lett. 39, 1853 (1998). Prepn of ester prodrug: M. N. Arimilli et al., Antiviral Chem. Chemother. 8, 557 (1997); idem et al., WO 9804569; eidem, US 5922695 (1998, 1999 both to Gilead Sci.). Antiretroviral activity in vitro: J. Balzarini et al., Biochem. Biophys. Res. Commun. 219, 337 (1996). Metabolism and pharmacokinetics of prodrugs: J.-P. Shaw et al., Pharm. Res. 14, 1824 (1997). Clinical trial in HIV-infected patients: J. E. Gallant et al., J. Am. Med. Assoc. 292, 191 (2004).

Teprenone CAS Registry Number: 6809-52-5 替普瑞酮

CAS Name: 6,10,14,18-Tetramethyl-5,9,13,17-nonadecatetraen-2-one
Additional Names: geranylgeranylacetone; GGATrademarks: Selbex (Eisai)
Percent Composition: C 83.57%, H 11.59%, O 4.84%
Literature References: Acyclic polyisoprenoid 2:3 mixture of (5Z,9E,13E) and all trans (5E,9E,13E) isomers. Prepn from geranylgeranyl bromide: L. Ruzicka, L. Castro, Helv. Chim. Acta 28, 590 (1945); from substituted acetylenes: K. Sato et al., J. Org. Chem. 35, 565 (1970). Anti-ulcer and toxicity studies: M. Murakami et al., Arzneim.-Forsch. 31, 799 (1981). In vivo effects on aspirin induced gastric ulcer: eidem, Jpn. J. Pharmacol. 32, 299 (1982); on stress induced gastric ulcer: eidem, ibid. 33, 549 (1983). Mechanism of action studies: Y. Nishizawa et al., Biochem. Biophys. Res. Commun. 103, 706 (1981); K. Oketani et al., Jpn. J. Pharmacol. 33, 593 (1983). Metabolism in rats: Y. Nishizawa et al., Xenobiotica 17, 575 (1987). Determn in serum by GC-MS: M. Tanaka et al., J. Chromatogr. 231, 301 (1982); by HPLC: T. Seki et al., ibid. 424, 410 (1988).

Betamipron CAS Registry Number: 3440-28-6 N-苯甲酰基-beta-丙氨酸

CAS Name: N-Benzoyl-b-alanine
Additional Names: 3-(benzoylamino)propionic acid; b-benzamidopropionic acid
Trademarks: CS-443
Percent Composition: C 62.17%, H 5.74%, N 7.25%, O 24.84%
Literature References: Acyl amino acid that inhibits active transport of carbapenem antibiotics in the renal cortex. See also panipenem. Prepn: F. H. Holm, Arch. Pharm. 242, 590 (1904); C. C. Barker, J. Chem. Soc. 1954, 317; J. Barluenga et al., Tetrahedron 45, 2183 (1989). Use as renal protectant: T. Shiokari et al., EP 226304; eidem, US 4757066 (1987, 1988 both to Sankyo). Crystal structure: N. Feeder, W. Jones, Acta Crystallogr. C50, 813 (1994). Nephroprotective effect: Y. Hirouchi et al., Jpn. J. Pharmacol. 63, 487 (1993). Mode of action: eidem, ibid. 66, 1 (1994). Pharmacokinetics: A. Kurihara et al., Antimicrob. Agents Chemother. 36, 1810 (1992).

Avasimibe CAS Registry Number: 166518-60-1 阿伐麦布

CAS Name: [[2,4,6-Tris(1-methylethyl)phenyl]acetyl]sulfamic acid 2,6-bis(1-methylethyl)phenyl ester
Additional Names: 2,6-diisopropylphenyl[(2,4,6-triisopropylphenyl)acetyl]sulfamatePercent Com...
Literature References: Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor. Prepn: H. T. Lee et al., WO 9426702; eidem, US 5491172 (1994, 1996 both to Warner Lambert). Scale up synthesis: G. J. Dozeman et al, Org. Process Res. Dev. 1, 137 (1997). ACAT inhibition studies: H. T. Lee et al., J. Med. Chem. 39, 5031 (1996). HPLC/MS/MS determn in plasma: W. W. Bullen et al., J. Pharm. Biomed. Anal. 17, 1399 (1998). Clinical evaluation in hyperlipidemia: W. Insull Jr. et al., Atherosclerosis 157, 137 (2001). Toxicology: D. G. Robertson et al., Toxicol. Sci. 59, 324 (2001). Reviews of development and therapeutic potential: R. Jones, Curr. Opin. Cardiovasc. Pulmon. Renal Invest. Drugs 1, 263-269 (1999); idem, ibid. 2, 274-278 (2000).

Sinefungin CAS Registry Number: 58944-73-3 西奈芬净

CAS Name: 6,9-Diamino-1-(6-amino-9H-purin-9-yl)-1,5,6,7,8,9-hexadeoxy-D-glycero-a-L-talo-decofuranuronic acid
Additional Names: Compd 57926; Antibiotic 32232RPPercent Composition: C 47.24%, H 6...
Literature References: Adenine-containing antibiotic produced by Streptomyces griseoleus NRRL 3739. Isoln: R. L. Hamill, M. M. Hoehn, US 3758681 (1973 to Lilly); eidem, J. Antibiot. 26, 463 (1973). Antifungal activity: R. S. Gordee, T. F. Butler, ibid. 466. Antiprotozoal activity: D. K. Dube et al., Am. J. Trop. Med. Hyg. 32, 31 (1983); A. Ferrante et al., Trans. R. Soc. Trop. Med. Hyg. 78, 837 (1984); P. Paolantonacci et al., Antimicrob. Agents Chemother. 28, 528 (1985); E. Zweygarth et al., Trop. Med. Parasitol. 37, 255 (1986); in vivo antileishmanial activity: J. L. Avila et al., Am. J. Trop. Med. Hyg. 43, 139 (1990). Synthesis: M. Geze et al., J. Am. Chem. Soc. 105, 7638 (1983); stereoselective synthesis: M. P. Maguire et al., J. Org. Chem. 55, 948 (1990). Inhibition of methyltransferase: R. T. Borchardt et al., Biochem. Biophys. Res. Commun. 89, 919 (1979).

Pentostatin CAS Registry Number: 53910-25-1 喷司他丁

CAS Name: (8R)-3-(2-Deoxy-b-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Additional Names: 2'-deoxycoformycin; DCF; 2'-dCFTrademarks: Nipent (SuperGen)
Percen...
Literature References: Adenosine deaminase inhibitor. Isoln from Streptomyces antibioticus and structure determn: P. W. K. Woo et al., J. Heterocycl. Chem. 11, 641 (1974). Isoln and purification: A. Ryder et al., DE 2517596; eidem, US 3923785 (both 1975 to Parke-Davis). Total synthesis: E. Chan et al., J. Org. Chem. 47, 3457 (1982). Preliminary biosynthetic study: J. C. Hanvey et al., Biochemistry 27, 5790 (1988). Inhibition of deaminases in vitro: T. Rogler-Brown et al., Biochem. Pharmacol. 27, 2289 (1978); C. Frieden et al., Biochem. Biophys. Res. Commun. 91, 278 (1979); in vivo: W. Plunkett et al., Biochem. Pharmacol. 28, 201 (1979). Toxicology study: J. F. Smyth et al., Cancer Chemother. Pharmacol. 1, 49 (1978). Clinical pharmacology: J. F. Smyth et al., ibid. 5, 93 (1980); P. P. Major et al., Blood 58, 91 (1981); F. J. Cummings et al., Clin. Pharmacol. Ther. 44, 501 (1988). Enzymatic determn in biological fluids: M. M. Chassin et al., Biochem. Pharmacol. 28, 1849 (1979); A. E. Staubus et al., ibid. 33, 1633 (1984). Clinical evaluation in hairy cell leukemia: J. B. Johnston et al., J. Natl. Cancer Inst. 80, 765 (1988). Brief review: P. O'Dwyer et al., Ann. Intern. Med. 108, 733 (1988). Review of clinical pharmacology and immunosuppressive effects: M. Higman et al., Expert Opin. Pharmacother. 5, 2605-2613 (2004).

Fludarabine CAS Registry Number: 21679-14-1 氟达拉滨

CAS Name: 9-b-D-Arabinofuranosyl-2-fluoro-9H-purin-6-amine
Additional Names: 9-b-D-arabinofuranosyl-2-fluoroadenine; 2-fluorovidarabine; 2-fluoro-9-b-D-arabinofuranosyladenine; 2-F-araAPercent ...
Literature References: Adenosine deaminase-resistant purine nucleoside antimetabolite. Prepn and in vitro cytotoxicity: J. A. Montgomery, K. Hewson, J. Med. Chem. 12, 498 (1969). Improved prepn: J. A. Montgomery et al., J. Heterocycl. Chem. 16, 157 (1979); J. A. Montgomery, US 4210745 (1980 to U.S. Dept. Health, Education and Welfare). Inhibition of DNA synthesis and in vivo antileukemic activity: R. W. Brockman et al., Biochem. Pharmacol. 26, 2193 (1977). Metabolized to 5¢-monophosphate: R. W. Brockman et al., Cancer Res. 40, 3610 (1980). HPLC determn in human leukemia cells: V. Gandhi et al., J. Chromatogr. 413, 293 (1987). Prepn of 5¢-monophosphate: J. A. Montgomery, A. T. Shortnacy, US 4357324 (1982 to U.S. Dept. of Health and Human Services). Pharmacokinetics in humans: M. R. Hersh et al., Cancer Chemother. Pharmacol. 17, 277 (1986). Evaluation of therapeutic efficacy and CNS toxicity in acute refractory leukemia: R. P. Warrell, Jr., E. Berman, J. Clin. Oncol. 4, 74 (1986); H. G. Chun et al., Cancer Treat. Rep. 70, 1225 (1986). Series of articles on pharmacology and therapeutic use: Semin. Oncol. 17, Suppl. 8, 1-78 (1990).

Deoxyepinephrine CAS Registry Number: 501-15-5 N-2-(3,4-二羟基苯基)乙基甲胺

CAS Name: 4-[2-(Methylamino)ethyl]-1,2-benzenediol
Additional Names: 4-[2-(methylamino)ethyl]pyrocatechol; 3,4-dihydroxyphenylethylamine; methyl[b-(3,4-dihydroxyphenyl)ethyl]amine; N-methyldopa...
Literature References: Adrenergic and dopamine receptor agonist; active metabolite of ibopamine, q.v. Prepd by heating HCl and 1-keto-6,7-dimethoxy-2-methyltetrahydroisoquinoline obtained from laudanosine or papaverine: Pyman, J. Chem. Soc. 95, 1266, 1610 (1909). Synthesis from veratrole: Kindler, Peschke, Arch. Pharm. 270, 340 (1932); Kindler, Hesse, ibid. 271, 439 (1933). From methylhomoveratrylamine: Buck, J. Am. Chem. Soc. 52, 4119 (1930); Bretschneider, Monatsh. Chem. 76, 335 (1947). Precursor in biosynthesis of epinephrine: W. F. Bridgers, S. Kaufman, J. Biol. Chem. 237, 526 (1962). Cardiovascular pharmacology: I. Martínez-Mir et al., Gen. Pharmacol. 31, 75 (1998). Comparison with 3,4-dihyroxybenzylamine in catecholamine analysis: H. He et al., J. Chromatogr. B 701, 115 (1997).