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

Oxidronic Acid CAS Registry Number: 15468-10-7 奥昔膦酸

CAS Name: (Hydroxymethylene)bisphosphonic acid
Additional Names: (hydroxymethylene)diphosphonic acid; HDP; HMDP
Percent Composition: C 6.26%, H 3.15%, O 58.33%, P 32.26%
Literature References: Bisphosphonate similar to etidronic acid, q.v. Prepn: O. T. Quimby, FR 1506840; idem, US 3422137 (1967, 1969 both to Procter Gamble); of sodium salt: idem et al., J. Org. Chem. 32, 4111 (1967). Prepn of 99mTc-complex: J. A. Bevan, EP 7676; idem, US 4247534 (1980, 1981 both to Procter Gamble); and osteotropic properties: T. S. T. Wang et al., J. Nucl. Med. 21, 767 (1980). Biodistribution: J. A. Bevan et al., ibid. 961. Radiochemical purity: W. Majewski et al., J. Nucl. Med. Technol. 11, 23 (1983). Clinical evaluation as skeletal imaging agent: P. A. Domstad et al., Radiology 136, 209 (1980). Diagnostic use in Paget's disease: A. Evans et al., Eur. J. Nucl. Med. 18, 757 (1991); for localization of bone metastases: F. Tenenbaum et al., ibid. 20, 1168 (1993).

Clodronic Acid CAS Registry Number: 10596-23-3 氯屈瞵酸

CAS Name: (Dichloromethylene)bisphosphonic acid
Additional Names: (dichloromethylene)diphosphonic acid; dichloromethanediphosphonic acid; Cl2MDP; DMDP
Percent Composition: C 4.90%, H 1.65%, ...
Literature References: Bisphosponate antiresorptive agent. Prepn and use as detergent additive: BE 672205 (1966 to Procter and Gamble), C.A. 67, 4040u (1967). Prepn: O. T. Quimby et al., J. Org. Chem. 32, 4111 (1967). Effect on hydroxyapatite durapatite, q.v., crystal aggregation: N. M. Hansen et al., Biochim. Biophys. Acta 451, 549 (1976); S. Bisaz et al., ibid. 560. HPLC determn in urine: V. Virtanen, L. H. J. Lajunen, J. Chromatogr. 617, 291 (1993). Symposium on therapeutic efficacy in neoplastic bone disease: Bone 8, Suppl. 1, S1-S86 (1987). Review of pharmacology and clinical efficacy in resorptive bone disease: G. L. Plosker, K. L. Goa, Drugs 47, 945-982 (1994). Clinical reduction of new metastases in breast cancer: I. J. Diel et al., N. Engl. J. Med. 339, 357 (1998).

HLö-7 CAS Registry Number: 120103-35-7 4-氨基甲酰-1-({[(4E)-2-[(E)-(羟基亚胺)甲基]-4-[(氧代铵基)亚甲基]-1(4H)-吡啶基]甲氧基}甲基)吡啶鎓二碘化物

CAS Name: 1-[[[4-(Aminocarbonyl)pyridinio]methoxy]methyl]-2,4-bis[(hydroxyimino)methyl]pyridinium diiodide
Additional Names: HLoe-7
Percent Composition: C 30.79%, H 2.93%, I 43.38%, N 11.97%...
Literature References: Bisquaternary Hagedorn oxime; acetylcholinesterase reactivator. In vitro reactivation of tabun and soman acetylcholinesterase inhibition: L. P. A. de Jong et al., Biochem. Pharmacol. 38, 633 (1989). Stability and decomposition: P. Eyer et al., Arch. Toxicol. 63, 59 (1989). Synthesis, pharmacology and toxicity: eidem, ibid. 66, 603 (1992). Pharmacokinetics: U. Spöhrer et al., ibid. 68, 480 (1994). Efficacy in nerve agent poisoning: B. P. C. Melchers et al., Pharmacol. Biochem. Behav. 49, 781 (1994). MS determn: P. A. D'Agostino et al., Rapid Commun. Mass Spectrom. 10, 805 (1996). Comparative reactivation studies in human acetylcholinesterase inhibition: F. Worek et al., Biochem. Pharmacol. 68, 2237 (2004).

Picrolichenic Acid CAS Registry Number: 466-34-2 6-羟基-2'-甲氧基-2,4'-二氧代-4,6'-二戊基螺[1-苯并呋喃-3,1'-环己[2,5]二烯]-5-羧酸

CAS Name: 6-Hydroxy-2'-methoxy-2,4'-dioxo-4,6'-dipentylspiro[benzofuran-3(2H),1'-[2,5]cyclohexadiene]-5-carboxylic acid
Additional Names: picrolichenin
Percent Composition: C 67.86%, H 6.83%...
Literature References: Bitter acidic principle of crustose lichen, Pertusaria amara (Ach.) Nyl., Pertusariaceae. Isoln: Alms, Ann. Pharm. 1, 61 (1832). Identity of picrolichenin and picrolichenic acid: Zopf, Ann. 321, 38 (1902). Isoln and structure: Wachmeister, Acta Chem. Scand. 12, 147 (1958). Synthesis: Davidson, Scott, J. Chem. Soc. 1961, 4075.

Oleuropein CAS Registry Number: 32619-42-4 橄榄苦苷

CAS Name: [2S-(2a,3E,4b)]-3-Ethylidene-2-(b-D-glucopyranosyloxy)-3,4-dihydro-5-(methoxycarbonyl)-2H-pyran-4-acetic acid 2-(3,4-dihydroxyphenyl)ethyl ester
Percent Composition: C 55.55%, H 5.97%...
Literature References: Bitter glucoside; first secoiridoid to be isolated. Isolation from olives and the leaves and bark of the olive tree, Olea europaea L., Oleaceae and structural studies: Panizzi et al., Gazz. Chim. Ital. 90, 1449 (1960); Beyerman et al., Bull. Soc. Chim. Fr. 1961, 1821; Shasha, Leibowitz, J. Org. Chem. 26, 1948 (1961). Isoln from the ripe fruits of Ligustrum lucidum and L. japonicum Thunb, Oleaceae: Inouye, Nishioka, Tetrahedron 28, 4231 (1972). Revised structure and stereochemistry: Inouye et al., Tetrahedron Lett. 1970, 2459. Pharmacology: Petkov, Manolov, Arzneim.-Forsch. 22, 1476 (1972). Partial synthesis: A. Bianco et al., J. Nat. Prod. 55, 760 (1992).

Isoquassin CAS Registry Number: 21293-20-9

Additional Names: Picrasmin
Percent Composition: C 68.02%, H 7.27%, O 24.71%
Literature References: Bitter principle from Jamaica quassia, Picrasma excelsa (Sw.) Planch., Simaroubaceae. Isoln: Clark, J. Am. Chem. Soc. 60, 1146 (1938). Identity of isoquassin and picrasmin: Adams, Whaley, ibid. 72, 375 (1950). Isomer of quassin, q.v.: Valenta et al., Tetrahedron 18, 1433 (1962).

Condurangin CAS Registry Number: 1401-98-5

Additional Names: Kondurangin
Literature References: Bitter principle from the bark of the Condurango vine, Marsdenia condurango Reichb. f., Asclepiadaceae, also known as eagle vine, mataperro, condor vine. Habit. Ecuador, Peru. Isoln: Korte, Korte, Z. Naturforsch. 10b, 223 (1955); Zechner, Zölss, Sci. Pharm. 24, 107 (1956). Separation of fractions: Cellarius, Zechner, ibid. 34, 10 (1966). Proposed structure of the aglycone, condurangogenin A: Tschesche et al., Tetrahedron 21, 1777, 1797 (1965); 23, 1461 (1967).

Picrotoxin CAS Registry Number: 124-87-8 木防己苦毒素

Trademarks: Cocculin
Percent Composition: C 59.80%, H 5.69%, O 34.52%
Literature References: Bitter principle isolated from the seed of Anamirta cocculus L. Wight Arn., Menispermaceae, also found in Tinomiscium philippinense Diels. Molecular compd of one mole picrotoxinin and one mole picrotin, q.q.v., into which it is readily separated. Extraction procedure: Clark, J. Am. Chem. Soc. 57, 1111 (1935). Chemical bibliography: Helv. Chim. Acta 32, 1859 (1949). Crystal and molecular structure: L. Dupont et al., Acta Crystallogr. B32, 2987 (1976). Toxicity study: I. Setnikar et al., J. Pharmacol. Exp. Ther. 128, 176 (1960).

Swertiamarin CAS Registry Number: 17388-39-5 獐牙菜苦苷

CAS Name: [4aR-(4aa,5b,6a)]-5-Ethenyl-6-(b-D-glucopyranosyloxy)-4,4a,5,6-tetrahydro-4a-hydroxy-1H,3H-pyrano[3,4-c]pyran-1-one
Additional Names: 4,4a,5,6-tetrahydro-4aa-hydroxy-1-oxo-5b-vinyl-1H...
Literature References: Bitter principle of Swertia japonica (Maxim.) Makino, Gentianaceae. Yields erythrocentaurin on hydrolysis with emulsin. Isoln: Kubota, Tomita, Chem. Ind. (London) 1958, 229; Inouye et al., Chem. Pharm. Bull. 18, 1856 (1970). Occurrence in gentianaceous plants: Inouye, Nakamura, J. Pharm. Sci. Japan 91, 755 (1971), C.A. 75, 95431b (1971). Structure: Kubota, Tomita, Tetrahedron Lett. 1961, 176; Bull. Chem. Soc. Jpn. 34, 1345 (1961); Koch et al., Bull. Soc. Chim. Fr. 1964, 405. Stereochemistry: Inouye et al., Tetrahedron Lett. 1968, 4429. Biosynthesis studies: Inouye et al., Chem. Pharm. Bull. 18, 2043 (1970).

Clavulanic Acid CAS Registry Number: 58001-44-8 克拉维酸

CAS Name: [2R-(2a,3Z,5a)]-3-(2-Hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acidPercent Composition: C 48.25%, H 4.55%, N 7.03%, O 40.17%
Literature References: b-Lactamase inhibitor. Antibiotic produced by Streptomyces clavuligerus; first reported naturally occurring fused b-lactam containing oxygen. Isoln: M. Cole et al., DE 2517316 (1975 to Beecham), C.A. 84, 72635t (1976); A. G. Brown et al., J. Antibiot. 29, 668 (1976). Structure, x-ray crystallography: T. T. Howarth et al., Chem. Commun. 1976, 266. Total synthesis of (±)-form: P. H. Bentley et al., ibid. 1977, 748, 905; eidem, Tetrahedron Lett. 1979, 1889. b-Lactamase inhibition and antibacterial spectrum: C. Reading, M. Cole, Antimicrob. Agents Chemother. 11, 852 (1977). Mechanism of action: B. G. Spratt et al., ibid. 12, 406 (1977). Antibacterial activity, pharmacology and clinical efficacy of combination with amoxicillin: A. P. Ball et al., Lancet 1, 620 (1980); R. N. Brogden et al., Drugs 22, 337-362 (1981). In vitro and in vivo synergism with ticarcillin: R. Sutherland et al., Am. J. Med. 79, Suppl. 5B, 13 (1985).