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

Di-tert-butyl Tricarbonate CAS Registry Number: 24424-95-1

CAS Name: Tricarbonic acid bis(1,1-dimethylethyl)ester
Percent Composition: C 50.38%, H 6.92%, O 42.70%
Literature References: Mild reagent which converts most primary amines quantitatively into their corresponding isocyanate. Prepn: C. S. Dean, D. S. Tarbell, Chem. Commun. 1969, 728; B. M. Pope et al., Org. Synth. 57, 45 (1977). Kinetic study: eidem, J. Org. Chem. 43, 2410 (1978). Use in prepn of isocyanates: H. W. I. Peerlings, E. W. Meijer, Tetrahedron Lett. 40, 1021 (1999); of polyurethanes: R. V. Versteegen et al., Angew. Chem. Int. Ed. 38, 2917 (1999).

Bis(pyridine)iodonium Tetrafluoroborate CAS Registry Number: 15656-28-7 双(吡啶)四氟硼化碘

CAS Name: Bis(pyridine)iodine(1+) tetrafluoroborate(1-)
Additional Names: Barluenga's reagent; IPy2BF4
Percent Composition: C 32.29%, H 2.71%, I 34.12%, N 7.53%, B 2.91%, F 20.43%
Literature References: Mild source of iodonium ions in organic synthesis. Prepn: J. Barluenga et al., Angew. Chem. Int. Ed. 24, 319 (1985). Oxidation of alcohols: idem et al., Chem. Eur. J. 10, 4206 (2004). Brief review: K. Muñiz, Synlett 1999, 1679. Review of iodination chemistry: J. Barluenga, Pure Appl. Chem. 71, 431-436 (1999).

Micranthine CAS Registry Number: 36104-64-0 防己索林

CAS Name: 6',7-Epoxy-6-methoxy-2-methyl-oxyacanthan-12'-ol
Percent Composition: C 74.43%, H 5.88%, N 5.11%, O 14.58%
Literature References: Minor alkaloid from bark of Daphnandra micrantha (Tul.) Benth., Monimiaceae. Isoln: Pyman, J. Chem. Soc. 105, 1679 (1914). Structure: Bick, Todd, ibid. 1950, 1606. Revised structure and stereochemistry: Bick et al., Tetrahedron Lett. 1972, 33. Biogenesis: I. Ralph, C. Bick, Heterocycles 16, 2105 (1981).

Cephalonic Acid CAS Registry Number: 18456-04-7 (6Z)-8-羟基-5-氧代菲奥波拉-3,6,19-三烯-25-酸

CAS Name: 8-Hydroxy-5-oxoophiobola-3,6,19-trien-25-oic acid
Additional Names: ophiobolin D
Percent Composition: C 74.96%, H 9.06%, O 15.98%
Literature References: Minor antibiotic metabolite produced by Cephalosporium caerulens. Exhibits weak activity against Staphylococcus aureus. Isolation, structure elucidation and physical data: Itai et al., Tetrahedron Lett. 1967, 4111; Nozoe et al., ibid. 4113. Crystal structure: Itai et al., Acta Crystallogr. 25B, 872 (1969). Synthetic studies on related compounds: P. C. Dutta, T. K. Das, Synth. Commun. 6, 253 (1976); W. G. Dauben, D. S. Hart, J. Org. Chem. 42, 922 (1977); R. K. Boeckman et al., ibid. 3630.

Codamine CAS Registry Number: 21040-59-5 (S)-1-[(3,4-二甲氧基苯基)甲基]-1,2,3,4-四氢-6-甲氧基-2-甲基异喹啉-7-醇

CAS Name: (1S)-1-[(3,4-Dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6-methoxy-2-methyl-7-isoquinolinol
Additional Names: 1,2,3,4-tetrahydro-6-methoxy-2-methyl-1-veratryl-7-isoquinolinol
Percen...
Literature References: Minor opium alkaloid. Constitutes about 0.003% of Turkish opium. Isoln: Hesse, Ann. 282, 213 (1894). Structure: Späth, Epstein, Ber. 59B, 2791 (1926). Synthesis: Schöpf, Thierfelder, Ann. 537, 143 (1939); Billek, Monatsh. Chem. 87, 106 (1956).

Protocatechuic Acid CAS Registry Number: 99-50-3 原儿茶酸

CAS Name: 3,4-Dihydroxybenzoic acid
Percent Composition: C 54.55%, H 3.92%, O 41.52%
Literature References: Minute amounts are found in wheat grains, in wheat seedlings, and in many other plants: L. Hörhammer, A. Scherm, Arch. Pharm. 288, 441 (1955). Prepd by the alkaline fusion of vanillin: Tiemann, Haarmann, Ber. 7, 617 (1874); Pearl, J. Am. Chem. Soc. 68, 2180 (1946); Org. Synth. coll. vol. III, 745 (1955).

Carbon Disulfide CAS Registry Number: 75-15-0 二硫化碳

Additional Names: Carbon bisulfide; dithiocarbonic anhydride
Percent Composition: C 15.77%, S 84.23%
Literature References: Minute amounts occur in coal tar and in crude petroleum. Prepd on an industrial scale by heating charcoal with vaporized sulfur; from sulfur and natural gas: Faith, Keyes Clark's Industrial Chemicals, F. A. Lowenheim, M. K. Moran, Eds. (Wiley-Interscience, New York, 4th ed., 1975) pp 224-229. Laboratory purification: Glemser in Handbook of Preparative Inorganic Chemistry vol. 1, G. Brauer, Ed. (Academic Press, New York, 2nd ed., 1963) p 652. Review of production and uses: Bushell, Chem. Ind. (London) 1961, 1465; R. W. Timmerman in Kirk-Othmer Encyclopedia of Chemical Technology vol. 4 (Wiley-Interscience, New York, 3rd ed., 1978) pp 742-757; of toxicology and human exposure: Toxicological Profile for Carbon Disulfide (PB97-121073, 1996) 252 pp.

Flosequinan CAS Registry Number: 76568-02-0 氟司喹南

CAS Name: 7-Fluoro-1-methyl-3-(methylsulfinyl)-4(1H)-quinolinone
Additional Names: flosequinonTrademarks: Manoplax (Boots)
Percent Composition: C 55.22%, H 4.21%, F 7.94%, N 5.85%, O 13.37%,...
Literature References: Mixed arterial and venous vasodilator. Prepn: R. V. Davies et al., DE 3011994; eidem, US 4302460 (1980, 1981 both to Boots). Pharmacology: J. G. Smith, G. T. Kinasewitz, J. Cardiovasc. Pharmacol. 8, 878 (1986); M. F. Sim et al., Br. J. Pharmacol. 94, 371 (1988). HPLC determn in plasma, serum and urine: M. B. Slegowski et al., J. Chromatogr. 425, 227 (1988). Pharmacokinetics and hemodynamics in humans: A. J. Cowley et al., J. Hypertens. 2, Suppl. 3, 547 (1984); R. D. Wynne et al., Eur. J. Clin. Pharmacol. 28, 659 (1985). Preliminary evaluation in hypertension: A. J. Cowley et al., ibid. 33, 203 (1987); in congestive heart failure: P. D. Kessler, M. Packer, Am. Heart J. 113, 137 (1987); P. D. Kessler et al., J. Cardiovasc. Pharmacol. 12, 6 (1988). Clinical study in chronic heart failure: A. J. Cowley et al., Br. Med. J. 297, 169 (1988).

Pindolol CAS Registry Number: 13523-86-9 吲哚洛尔

CAS Name: 1-(1H-Indol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol
Additional Names: 4-[2-hydroxy-3-(isopropylamino)propoxy]indole; prinodololTrademarks: Betapindol (Helvepharm); Blocklin L (Sh...
Literature References: Mixed b-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Prepn: NL 6601040; F. Troxler, A. Hofmann, US 3471515 (1966, 1969 both to Sandoz). HPLC determn in plasma: H. Smith, J. Chromatogr. 415, 95 (1987). Symposia on cardiovascular pharmacology and clinical studies: Am. Heart J. 104, Suppl. 2, pt. 2, 333-520 (1982); Br. J. Clin. Pharmacol. 13, Suppl. 2, 143S-450S (1982). Effect on serotonin levels in rat brain: L. J. Dreshfield et al., Neurochem. Res. 21, 557 (1996). Clinical trial with fluoxetine, q.v., in depression: V. Pérez et al., Lancet 349, 1594 (1997).

Dotarizine CAS Registry Number: 84625-59-2 多他利嗪

CAS Name: 1-(Diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazinePercent Composition: C 78.70%, H 7.74%, N 6.33%, O 7.23%
Literature References: Mixed calcium channel blocker and serotonin (5-HT2) receptor antagonist. Prepn: R. Foguet et al., EP 97340; eidem, US 4883797 (1984, 1989 both to Ferrer); S. Gubert et al., Arzneim.-Forsch. 37, 1103 (1987). Clinical pharmacokinetics and tolerability: M. Farré et al., Methods Find. Exp. Clin. Pharmacol. 19, 343 (1997). Cerebrovascular study in goats: G. Torregrosa et al., Arzneim.-Forsch. 49, 668 (1999); in rabbits: N. Kuridze et al., J. Neurol. Sci. 175, 13 (2000). Mechanism of blockade: A. Ruiz-Nuno et al., Eur. J. Pharmacol. 411, 289 (2001).