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

Imipenem CAS Registry Number: 74431-23-5; 64221-86-9 (anhydrous) 亚胺培南(一水物)

CAS Name: (5R,6S)-6-[(1R)-1-Hydroxyethyl]-3-[[2-[(iminomethyl)amino]ethyl]thio]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate
Additional Names: N-formimidoylthienamycin mono...
Literature References: Extremely broad-spectrum semi-synthetic antibiotic; first stable derivative of thienamycin, q.v. Prepn: W. J. Leanza et al., J. Med. Chem. 22, 1435 (1979); T. W. Miller, EP 6639 (1980 to Merck Co.), C.A. 93, 155845y (1980); B. G. Christensen et al., US 4194047 (1980 to Merck Co.). Totally synthetic prepn without formation of thienamycin: I. Shinkai et al., Tetrahedron Lett. 23, 4903 (1982). HPLC determn in serum: C. M. Myers, J. L. Blumer, Antimicrob. Agents Chemother. 26, 78 (1984). Series of articles on in vitro activity, pharmacokinetics, clinical efficacy of combination with cilastatin sodium, q.v., a renal dehydropeptidase I inhibitor: J. Antimicrob. Chemother. 12, Suppl. D, 1-155 (1983); Rev. Infect. Dis. 7, Suppl. 3, S389-S536 (1985); Am. J. Med. 78, Suppl. 6A, 1-167 (1985); Infection 14, Suppl. 2, S111-S180 (1986). Comprehensive description: E. R. Oberholtzer, Anal. Profiles Drug Subs. 17, 73-114 (1988).

Tipifarnib CAS Registry Number: 192185-72-1; 192185-68-5 (unspecified stereo) 替吡法尼

CAS Name: 6-[(R)-Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinoneTrademarks: Zarnestra (Janssen)
Percent Composition: C 66.26%, H 4.53%, Cl ...
Literature References: Farnesyl transferase inhibitor. Prepn: M. G. Venet et al., WO 9721701; eidem, US 6037350 (1997, 2000 both to Janssen). Review of syntheses: P. R. Angibaud et al., Eur. J. Org. Chem. 2004, 479-486. Inhibition of farnesyl protein transferase and antitumor effects in vivo: D. W. End et al., Cancer Res. 61, 131 (2001). Clinical pharmacology and pharmacokinetics: J. Zujewski et al., J. Clin. Oncol. 18, 927 (2000). Accelerator mass spec determn in biological samples: R. C. Garner et al., Drug Metab. Dispos. 30, 823 (2002). Clinical evaluation in hematologic malignancies: J. Cortes et al., Blood 101, 1692 (2003). Review of clinical experience: P. Norman, Curr. Opin. Invest. Drugs 3, 313-319 (2002).

Fluroxene CAS Registry Number: 406-90-6 三氟乙烯醚

CAS Name: (2,2,2-Trifluoroethoxy)ethene
Additional Names: 2,2,2-trifluoroethyl vinyl ether
Trademarks: Fluoromar (formerly) (Ohio Med.)
Percent Composition: C 38.11%, H 4.00%, F 45.21%, O...
Literature References: First clinical fluorinated inhalation anesthetic agent. Prepd (not claimed): J. G. Shukys, US 2830007; P. W. Townsend, US 2870218 (1958, 1959 to Air Reduction). Anesthetic action: J. C. Krantz, Jr. et al., J. Pharmacol. Exp. Ther. 108, 488 (1953). Review of metabolism and toxicity: V. Fiserova-Bergerova, Environ. Health Perspect. 21, 225-230 (1977); L. S. Kaminsky, J. M. Fraser, Crit. Rev. Toxicol. 19, 87-112 (1988).

Morphenol CAS Registry Number: 519-56-2 菲并[4,5-bcd]呋喃-3-醇

CAS Name: Phenanthro[4,5-bcd]furan-3-ol
Additional Names: 3-hydroxy-4,5-oxidophenanthrene; 3-hydroxy-4,5-phenanthrylene oxide
Percent Composition: C 80.76%, H 3.87%, O 15.37%
Literature References: First described by Vongerichten, Ber. 30, 2439 (1897). Prepn from morphine: Mosettig, Meitzner, J. Am. Chem. Soc. 56, 2738 (1934). Approach to synthesis: Dendy et al., J. Chem. Soc. 1963, 4040.

Monsel's Solution CAS Registry Number: 1310-45-8 碱式硫酸铁

Additional Names: Ferric subsulfate solution
Literature References: First described in 1856 by L. Monsel. Prepd by oxidizing ferrous sulfate with nitric acid in the presence of sulfuric acid. Prepn: W. Procter, Jr., Am. J. Pharm. 31, 403 (1859). Review of chemistry and mechanism of action: E. Epstein, H. I. Maibach, Arch. Dermatol. 90, 226-228 (1964); of hemostatic applications: A. B. Jetmore et al., Dis. Colon Rectum 36, 866-867 (1993); of history: A. P. Garrett et al., J. Lower Genital Tract Dis. 6, 225-227 (2002).

Oxaprozin CAS Registry Number: 21256-18-8 奥沙普秦

CAS Name: 4,5-Diphenyl-2-oxazolepropanoic acid
Additional Names: b-(4,5-diphenyloxazol-2-yl)propionic acidTrademarks: Alvo (Taisho); Daypro (Pfizer)
Percent Composition: C 73.71%, H 5.15%, N...
Literature References: First description of anti-inflammatory properties: K. Brown et al., Nature 219, 164 (1968). Prepn: FR 2001036 (1969 to Inst. Farm. Serono), C.A. 72, 66930w (1970); K. Brown, GB 1206403 and US 3578671 (1970, 1971 both to Wyeth). Biochemical properties: M. W. Whitehouse et al., Biochem. Pharmacol. 20, 2309 (1971). Metabolism: F. W. Janssen et al., Drug Metab. Dispos. 6, 465 (1978). Pharmacology: D. A. Shriver et al., Toxicol. Appl. Pharmacol. 42, 75 (1977); F. Awouters et al., J. Pharm. Pharmacol. 30, 41 (1978). Clinical studies: R. Jamar, J. Dequeker, Curr. Med. Res. Opin. 5, 433 (1978); J. A. Hubsher et al., J. Int. Med. Res. 7, 69 (1979); eidem, Arthritis Rheum. 25, S117 (1982). Protein binding and clearance: C. A. Homon et al., Agents Actions 12, 211 (1982). Symposium on pharmacology and clinical efficacy: Semin. Arthritis Rheum. 15, Suppl. 3, 1-107 (1986). Review of mechanism of action and clinical efficacy: F. Dallegri et. al., Expert Opin. Pharmacother. 6, 777-785 (2005).

Ergothioneine CAS Registry Number: 497-30-3 麦角硫因

CAS Name: (aS)-a-Carboxy-2,3-dihydro-N,N,N-trimethyl-2-thioxo-1H-imidazole-4-ethanaminium inner salt
Additional Names: [1-carboxy-2-[2-mercaptoimidazol-4-yl]ethyl]trimethylammonium hydroxide in...
Literature References: First discovered in the sclerotia of the ergot fungus, Claviceps purpurea, by Tanret, J. Pharm. Chim. 30, 145 (1909). Has since been found to occur in blood, semen and various mammalian tissues, principally liver and kidneys. Biosynthesis from histidine by Claviceps purpurea cultures: Heath, Wildy, Nature 179, 196 (1957); also produced by Neurospora crassa: Melville et al., Fed. Proc. 15, 314 (1956). Chemical synthesis: Heath et al., J. Chem. Soc. 1951, 2215. Occurrence in the Linulus polyphemus L. (king crab): Ackermann, List, Z. Physiol. Chem. 313, 30 (1958). Review: Melville, Vitam. Horm. 17, 155 (1959).

Apiose CAS Registry Number: 639-97-4 3-C-羟基甲基-d-丙三醇-四糖

CAS Name: D-Apiose
Additional Names: tetrahydroxyisovaleraldehyde; 3-C-(hydroxymethyl)-D-glyceroaldotetrose
Percent Composition: C 40.00%, H 6.71%, O 53.29%
Literature References: First found in parsley in which it occurs as the flavinoid glycoside apiin, q.v. Isoln from apiin: Vongerichten, Ann. 318, 126 (1901); 321, 74 (1902); Hemming, Ollis, Chem. Ind. (London) 1953, 85. From the rubber plant, Hevea brasiliensis, Euphorbiaceae: Patrick, Nature 178, 216 (1956). Discussion of structure and isoln from the Australian marine plant Posidonia australis Kon., Potamogetonaceae: Bell, Methods in Carbohydrate Chemistry vol. I (Academic Press, New York, 1962) pp 260-263. Synthesis: Gorin, Perlin, Can. J. Chem. 36, 480 (1958); Khalique, J. Chem. Soc. 1962, 2515; Ezekiel et al., Tetrahedron Lett. 1969, 1635. Synthesis of L-form: Weygand, Schmiechen, Ber. 92, 535 (1959); of DL-form: Kinoshita, Miwa, Carbohydr. Res. 28, 175 (1973); Y. Araki et al., ibid. 58, C4 (1977); of D- and L-forms: P. Ho, Can. J. Chem. 57, 381 (1979). Chemistry, configuration and synthesis studies: Williams, Jones, ibid. 42, 69 (1964); Hulyalker et al., ibid. 43, 2085 (1965). Review: Watson, Orenstein, Adv. Carbohydr. Chem. Biochem. 31, 135-184 (1975).

Okadaic Acid CAS Registry Number: 78111-17-8 冈田(软海绵)酸

CAS Name: 9,10-Deepithio-9,10-didehydroacanthifolicin
Additional Names: halochondrine A
Percent Composition: C 65.65%, H 8.51%, O 25.84%
Literature References: First ionophoric polyether identified in marine organisms; isolated from marine black sponges, Halichondria (okadai or melanodocia). Tumor promoting cytotoxin associated with diarrhetic seafood poisoning. Isoln: K. Tachibana et al., J. Am. Chem. Soc. 103, 2469 (1981). Total synthesis: M. Isobe et al., Tetrahedron 43, 4767 (1987). Contractile effects: S. Shibata et al., J. Pharmacol. Exp. Ther. 223, 135 (1982). Inhibition of protein phosphatases: A. Takai et al., FEBS Lett. 217, 81 (1987); C. Bialojan, A. Takai, Biochem. J. 256, 283 (1988). Tumor promoting activity: M. Suganuma et al., Proc. Natl. Acad. Sci. USA 85, 1768 (1988). Review of mechanism of action and use as a probe for cellular regulation: P. Cohen et al., Trends Biochem. Sci. 15, 98-102 (1990); A. Schönthal, New Biol. 4, 16-21 (1992). Review of tumor promoting activity: H. Fujiki, M. Suganuma, J. Biochem. 115, 1-5 (1994).

Syringin CAS Registry Number: 118-34-3 紫丁香酚甙; 刺五加甙B

CAS Name: (E)-4-(3-Hydroxy-1-propenyl)-2,6-dimethoxyphenyl-b-D-glucopyranoside
Additional Names: 4-(3-hydroxypropenyl)-2,6-dimethoxyphenyl-D-glucoside; syringoside; ligustrin; lilacin; methoxyc...
Literature References: First isolated by Meillet in 1841 from bark of Syringa vulgaris L. (lilac): Ann. 40, 319 (1841). Prepn: Pauly, Strassberger, Ber. 62, 2277 (1929); Freudenberg, Schraube, Ber. 88, 16 (1955). Isoln from lilac bark: Freudenberg et al., Ber. 84, 472 (1951); from various plants: Plouvier, Compt. Rend. 254,4196 (1962); from cambial sap of spruce: Freudenberg, Harkin, Phytochemistry 2, 189 (1963).