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

Etamycin CAS Registry Number: 299-20-7 宜他霉素A

Additional Names: Etamycin A; neoviridogrisein IV; viridogrisein
Percent Composition: C 60.12%, H 7.11%, N 12.75%, O 20.02%
Literature References: Monocyclic peptide lactone antibiotic produced by Streptomyces griseus and allied Streptomyces spp., which shows activity vs gram positive bacteria, Mycobacterium tuberculosis and some fungi. Obtained together with griseoviridin. Production and isoln: B. Heinemann et al., Antibiot. Annu. 1954-55, 728; Q. R. Bartz et al., ibid. 777. Pharmacology: H. L. Dickison et al., ibid. 733. Chemical studies: T. H. Haskell et al., ibid. 784. Biological studies: J. Ehrlich et al., ibid. 790. Structure: Sheehan et al., J. Am. Chem. Soc. 80, 3349 (1958). Confirmation of structure: Arnold et al., J. Chem. Soc. 1958, 4466. Prodn with griseoviridin: Q. R. Bartz et al., US 3023204 (1962 to Parke, Davis). Total synthesis: Sheehan, Ledis, J. Am. Chem. Soc. 95, 875 (1973). Mode of action: Garcia-Mendoza, Biochim. Biophys. Acta 97, 94 (1965). Mass spectra data: Rozynov et al., Zh. Obshch. Khim. 39, 891 (1969). Prodn of congeners by S. griseoviridus: C. Chopra et al., J. Antibiot. 32, 392 (1979). Biosynthetic studies of neoviridogriseins, homologs of etamycin: Y. Akumura et al., ibid. 575, 1002, 1130.

Potassium Thiocarbonate CAS Registry Number: 26750-66-3 三硫代碳酸钾

Additional Names: Potassium sulfocarbonate; potassium trithiocarbonate
Percent Composition: C 6.44%, K 41.95%, S 51.61%
Literature References: Monograph: K. N. Johri, Chemical Analysis without H2S using Potassium Trithiocarbonate (Asia Pub., New York, 1963) 107 pp.

Potassium Triiodide CAS Registry Number: 7790-42-3

Percent Composition: I 90.69%, K 9.31%
Literature References: Monohydrate prepd by adding the stoichiometric amount of iodine to a hot soln of KI and cooling to 0°: H. L. Wells, H. L. Wheeler, Z. Anorg. Allg. Chem. 1, 453 (1892); H. W. Foote, W. C. Chalker, J. Am. Chem. Soc. 39, 565 (1908). Prepn of anhydrous: N. S. Grace, J. Chem. Soc. 1931, 594.

Tetrafluoroethylene CAS Registry Number: 116-14-3 四氟乙烯

CAS Name: Tetrafluoroethene
Additional Names: perfluoroethene; TFE
Percent Composition: C 24.02%, F 75.98%
Literature References: Monomer of the plastic, polytetrafluoroethylene, q.v. Prepn: O. Ruff, O. Bretschneider, Z. Anorg. Allg. Chem. 210, 173 (1933). Structural study: T. T. Broun, R. L. Livingston, J. Am. Chem. Soc. 74, 6084 (1952). Physical properties: M. M. Renfrew, E. E. Lewis, Ind. Eng. Chem. 38, 870 (1946). Addition reactions: D. D. Coffman et al., J. Org. Chem. 14, 747 (1949). Thermodynamics and kinetics of mfr by pyrolysis of chlorodifluoromethane: P. B. Chinoy, P. D. Sunavala, Ind. Eng. Chem. Res. 26, 1340 (1987). Review of mfr: Y. Venkateswarlu, P. S. Murti, Chem. Process. Eng. 4, 25-36 (1970); of chemistry: M. Saijwani, Dinkar, Labdev J. Sci. Tech. 9-A, 1-12 (1971); of toxicology: G. L. Kennedy, Jr., Crit. Rev. Toxicol. 21, 149-170 (1990).

PhIP CAS Registry Number: 105650-23-5 2-氨基-1-甲基-6-苯基咪唑[4,5-b]吡啶

CAS Name: 1-Methyl-6-phenyl-1H-imidazo[4,5-b]pyridin-2-amine
Additional Names: 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine
Percent Composition: C 69.62%, H 5.39%, N 24.98%
Literature References: Most abundant of the mutagenic heterocyclic amines found in well-cooked meat and fish. Isoln from fried ground beef: J. S. Felton et al., Carcinogenesis 7, 1081 (1986). Synthesis: M. G. Knize, J. S. Felton, Heterocycles 24, 1815 (1986); T. Choshi et al., J. Org. Chem. 58, 7952 (1993); F. S. Bavetta et al., Tetrahedron Lett. 44, 7793 (1997). Mutagenicity in Chinese hamster ovary cells: L. H. Thompson et al., Mutagenesis 2, 483 (1987). Evaluation of carcinogenic risk: IARC Monographs 56, 229-242 (1993). Review of bioavailability, content in foods, metabolism: N. J. Gooderham et al., Br. J. Clin. Pharmacol. 42, 91-98 (1996). Correlation of dietary intake with breast cancer risk: R. Sinha et al., J. Natl. Cancer Inst. 92, 1352 (2000).

a -Tocopherol CAS Registry Number: 59-02-9 维生素E油

CAS Name: (2R)-3,4-Dihydro-2,5,7,8-tetramethyl-2-[(4R,8R)-4,8,12-trimethyltridecyl]-2H-1-benzopyran-6-ol
Additional Names: (+)-2,5,7,8-tetramethyl-2-(4',8',12'-trimethyltridecyl)-6-chromanol; R...
Literature References: Most bioactive of the naturally occurring forms of vitamin E, q.v. Richest sources are green vegetables, grains, and oils, particularly palm, safflower and sunflower oils. Isoln from wheat germ: H. M. Evans et al., J. Biol. Chem. 113, 319 (1936). Structure: E. Fernholz, J. Am. Chem. Soc. 59, 1154 (1937); 60, 700 (1938). Synthesis of dl-form: P. Karrer et al., Helv. Chim. Acta 21, 520, 820 (1938); F. Bergel et al., J. Chem. Soc. 1938, 1382. Distillation from vegetable oils and prepn of esters: J. G. Baxter et al., J. Am. Chem. Soc. 918 (1943). Prepn of crystalline natural form: C. D. Robeson, ibid. 1660; of crystalline acetate: idem, ibid. 64, 1487 (1942). Abs config of natural a-tocopherol: H. Mayer et al., Helv. Chim. Acta 46, 963 (1963). Stereoselective synthesis: K.-K. Chan et al., J. Org. Chem. 43, 3435 (1978). Total synthesis of all 8 stereoisomers: N. Cohen et al., Helv. Chim. Acta 64, 1158 (1981). Clinical trial in Alzheimer's disease: M. Sano et al., N. Engl. J. Med. 336, 1216 (1997); to improve immune function in healthy elderly: S. N. Meydani et al., J. Am. Med. Assoc. 277, 1380 (1997). Review of bioavailability from vitamin E supplements: M. G. Traber, BioFactors 10, 115-120 (1999). Review of clinical trials in heart disease: W. A. Pryor, Free Radical Biol. Med. 28, 141-164 (2000).

b -Carotene CAS Registry Number: 7235-40-7 β-胡萝卜素

CAS Name: b,b-Carotene
Trademarks: Carotaben (Hermal); Provatene (Microbio); Solatene (Roche)
Percent Composition: C 89.49%, H 10.51%
Literature References: Most important of the provitamins A. Widely distributed in the plant and animal kingdom. In plants it occurs almost always together with chlorophyll. Isoln from carrots: Willstätter, Escher, Z. Physiol. Chem. 64, 47 (1910); Kuhn, Lederer, Ber. 64, 1349 (1931); Barnett et al., US 2848508 (1958). Chromatography: Karrer, Walker, Helv. Chim. Acta 16, 641 (1933). Structure: Willstätter, Mieg, Ann. 355, 1 (1907); Zechmeister et al., Ber. 61, 566 (1928); 66, 123 (1933); Karrer et al., Helv. Chim. Acta 12, 1142 (1929); 13, 1084 (1930); 14, 1033 (1931); Kuhn, Brockmann, Ber. 65, 894 (1932); 66, 1319 (1933); 67, 1408 (1934); Ann. 516, 95 (1935). Crystal structure: Sterling, Acta Crystallogr. 17, 1224 (1964). Synthesis: Milas et al., J. Am. Chem. Soc. 72, 4844 (1950); Karrer, Eugster, Compt. Rend. 250, 1920 (1950); Inhoffen et al., Chem. Ztg. 74, 285, 309 (1950); Surmatis, Ofner, J. Org. Chem. 26, 1171 (1961); Rüegg et al., Helv. Chim. Acta 44, 985 (1961); Bestmann et al., Ann. 1973, 760; Fischli, Mayer, Helv. Chim. Acta 58, 1584 (1975). Industrial mfg procedure: Isler et al., Helv. Chim. Acta 39, 249 (1956); Isler et al., US 2917539 (1959 to Hoffmann-La Roche). Microbial production by Choanephora trispora: Zajic, US 2959521; US 2959522 and US 3128236 (1960, 1960 and 1964, all to Grain Processing); Miescher, US 3001912 (1961 to C.S.C.). Review: Fleming, Selected Organic Syntheses (John Wiley, London, 1973) pp 70-74.

Ergosterol CAS Registry Number: 57-87-4 麦角固醇; 麦角甾醇

CAS Name: (3b,22E)-Ergosta-5,7,22-trien-3-ol
Additional Names: ergosta-5:6,7:8,22:23-trien-3-ol; ergosterin
Percent Composition: C 84.78%, H 11.18%, O 4.03%
Literature References: Most important of the provitamins D. Usually obtained from yeast which synthesizes it from simple sugars such as glucose. Damp yeast yields about 2.5% ergosterol, the variety of the yeast being very important. Isoln procedure: Green et al., US 3006932 (1961 to Vitamins Ltd.). When irradiated with uv light, ergosterol develops powerful vitamin D2, q.v., activity. Askew et al., in England and Windaus and collaborators in Germany isolated the antirachitic vitamin D2. The main irradiation products of ergsterol are lumisterol®tachysterol®vitamin D2. Structure: Chuang, Ann. 500, 270 (1933). Oxidation products: Fuerst, Arch. Pharm. 300, 144 (1967).

Linalyl Acetate CAS Registry Number: 115-95-7 乙酸芳樟酯

CAS Name: 3,7-Dimethyl-1,6-octadien-3-yl acetate
Trademarks: Bergamol (Synfleur)
Percent Composition: C 73.43%, H 10.27%, O 16.30%
Literature References: Most valuable constituent of bergamot and lavender oils, also found in many other volatile oils.

Zosuquidar CAS Registry Number: 167354-41-8 (6R,7R)-7-[[2-[2-(氨基甲基)苯基]乙酰]氨基]-3-[[1-(羧甲基)四唑-5-基]硫甲基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸

CAS Name: (aR)-4-[(1aa,6a,10ba)-1,1,-Difluoro-1,1a,6,10b-tetrahyrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-a-[(5-quinolinyloxy)methyl]-1-piperazineethanol
Additional Names: (2R)-anti-5-[3-[4-...
Literature References: Multidrug resistance (MDR) modulator; selective inhibitor of P-glycoprotein (P-gp), q.v. Prepn: J. R. Pfister, D. L. Slate, WO 9424107; eidem, US 5654304 (1994, 1997 both to Syntex); J. R. Pfister et al., Bioorg. Med. Chem. Lett. 5, 2473 (1995). Improved synthesis: C. J. Barnett et al., J. Org. Chem. 69, 7653 (2004). Effect on multidrug resistant cell lines: L. J. Green et al., Biochem. Pharmacol. 61, 1393 (2001). Specificity for P-gp: R. L. Shepard et al., Int. J. Cancer 103, 121 (2003). Clinical pharmacology and pharmacokinetics in patients with advanced malignancies: E. H. Rubin et al., Clin. Cancer Res. 8, 3710 (2002). Effect on pharmacokinetics of doxorubicin: S. Callies et al., Cancer Chemother. Pharmacol. 51, 107 (2003).