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

Lecithins CAS Registry Number: 8002-43-5 大豆磷脂

Additional Names: Phosphatidylcholine
Trademarks: Lecithol; Vitellin; Kelecin; Granulestin
Literature References: Phosphatides found in all living organisms (plants and animals). Significant constituent of nervous tissue and brain substance. A mixture of the diglycerides of stearic, palmitic, and oleic acids, linked to the choline ester of phosphoric acid. Commercial grades contain 2.2% P. Isoln from eggs: Sinclair, Can. J. Res. 26B, 777 (1948). Product of commerce is predominantly soybean lecithin obtained as a by-product in the manuf of soybean oil: Stanley in K. S. Markley, Soybeans vol. II (Interscience, New York, 1951) pp 593-647. Soybean lecithin contains palmitic acid 11.7%, stearic 4.0%, palmitoleic 8.6%, oleic 9.8%, linoleic 55.0%, linolenic 4.0%, C20 to C22 acids (includes arachidonic) 5.5%. Synthesis of a mixed acid a-lecithin: de Haas, van Deenen, Tetrahedron Lett. 1960 (no. 9), 1. Synthetic L-a-(distearoyl)lecithin is identical with hydrogenated egg yolk lecithin and L-a-(dipalmitoyl)lecithin is identical with colfosceril palmitate, q.v., a natural phosphatide of brain, lung, and spleen. Commercial grades of natural lecithin are reported to contain a potent vasodepressor substance: McQuarrie, Andersen, US 2931818 (1960 to Cutter Labs.). Comprehensive monograph: G. B. Ansell, J. N. Hawthorne, Phospholipids (Elsevier, New York, 1964) 439 pp; A. Wendel, "Lecithin" in Kirk-Othmer Encyclopedia of Chemical Technology vol. 15 (Wiley-Interscience, New York, 4th ed., 1995) pp 192-210.

Fosinopril CAS Registry Number: 98048-97-6 福辛普利

CAS Name: (4S)-4-Cyclohexyl-1-[[(R)-[(1S)-2-methyl-1-(1-oxopropoxy)propoxy](4-phenylbutyl)phosphinyl]acetyl]-L-proline
Additional Names: (4S)-4-cyclohexyl-1-[[[(RS)-1-hydroxy-2-methylpropoxy](4...
Literature References: Phosphinic acid containing angiotensin converting enzyme (ACE) inhibitor. Prepn: E. W. Petrillo, Jr., US 4337201 (1982 to Squibb); of active diacid form: J. Krapcho et al., J. Med. Chem. 31, 1148 (1988). Metabolism and pharmacokinetics: S. M. Singhvi et al., Br. J. Clin. Pharmacol. 25, 9 (1988). GC determn of diacid: M. Jemal et al., J. Chromatogr. 345, 299 (1985). Clinical trial in hypertension: P. A. Sullivan et al., Am. J. Hypertens. 1, 280S (1988). Brief description: E. W. Petrillo, Jr., et al., Clin. Exp. Theory Prac. A9, 235 (1987). Series of articles on pharmacology, pharmacokinetics, and clinical experience: Drug Invest. 3, Suppl. 4, 1-53 (1991).

Cilostazol CAS Registry Number: 73963-72-1 西洛他唑

CAS Name: 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone
Additional Names: 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydrocarbostyril; 6-[4-(1-cyclohexyl-5-te...
Literature References: Phosphodiesterase (PDE III) inhibitor; induces vasodilation and inhibits platelet aggregation. Prepn: BE 878548; T. Nishi, K. Nakagawa, US 4277479 (1979, 1981 both to Otsuka); T. Nishi et al., Chem. Pharm. Bull. 31, 1151 (1983). Physical properties: T. Shimizu et al., Arzneim.-Forsch. 35, 1117 (1985). HPLC determn in plasma: H. Akiyama et al., J. Chromatogr. 338, 456 (1985). Acute toxicity study: G. Nomura et al., Iyakuhin Kenkyu 16, 1200 (1985), C.A. 104, 102207f (1986). Clinical pharmacokinetics: A. Suri et al., J. Clin. Pharmacol. 38, 144 (1998). Clinical evaluation to prevent stent thrombosis: S.-W. Park et al., Am. J. Cardiol. 84, 511 (1999); to prevent restenosis after angioplasty: E. Tsuchikane et al., Circulation 100, 21 (1999). Review of pharmacology and clinical efficacy in intermittent claudication: E. M. Sorkin, A. Markham, Drugs Aging 14, 63-71 (1999).

Dipyridamole CAS Registry Number: 58-32-2 双嘧达莫

CAS Name: 2,2',2'',2'''-[(4,8-Di-1-piperidinylpyrimido[5,4-d]pyrimidine-2,6-diyl)dinitrilo]tetrakisethanol
Additional Names: 2,6-bis(diethanolamino)-4,8-dipiperidinopyrimido-[5,4-d]pyrimidineTr...
Literature References: Phosphodiesterase inhibitor that reduces platelet aggregation; also acts as a coronary vasodilator. Prepn: GB 807826; F. G. Fischer, et al., US 3031450 (1959, 1962 both to Thomae). Activity studies: Saraf, Seth, Indian J. Physiol. Pharmacol. 15, 135 (1971). Toxicological study: F. Takenaka et al., Arzneim.-Forsch. 22, 892 (1972). Symposium on pharmacology and clinical experience as antithrombotic: Thromb. Res. 60, Suppl. 12, 1-99 (1990). Review of use as pharmacological stress agent in echocardiography: M. B. Buchalter et al., Postgrad. Med. J. 66, 531-535 (1990); in 201Tl cardiac imaging: S. G. Beer et al., Am. J. Cardiol. 67, Suppl., 18D-26D (1991).

Anagrelide CAS Registry Number: 68475-42-3 阿那格雷

CAS Name: 6,7-Dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one
Additional Names: 6,7-dichloro-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one
Percent Composition: C 46.90%, H 2.76%, C...
Literature References: Phosphodiesterase inhibitor with antiplatelet activity. Prepn: W. N. Beverung, A. Partyka, US 3932407; US RE 31617; T. A. Jenks et al., US 4146718 (1976, 1984, 1979 all to Bristol-Myers); H. Yamaguchi, F. Ishikawa, J. Heterocycl. Chem. 18, 67 (1981). Antithrombotic and platelet aggregation inhibiting properties: J. S. Fleming, J. P. Buyniski, Thromb. Res. 15, 373 (1979). Mode of action studies: S. S. Tang, M. M. Frojmovic, J. Lab. Clin. Med. 95, 241 (1980); S. Seiler et al., J. Pharmacol. Exp. Ther. 243, 767 (1987). GC-MS determn in human plasma: E. H. Kerns et al., J. Chromatogr. 416, 357 (1987). Clinical reduction of platelet counts: W. A. Andes et al., Thromb. Haemostasis 52, 325 (1984). Clinical trials to control thrombocytosis in chronic myeloproliferative diseases: M. N. Silverstein et al., N. Engl. J. Med. 318, 1292 (1988); Anagrelide Study Group, Am. J. Med. 92, 69 (1992). Review of pharmacology and clinical experience: P. E. Petrides, Expert Opin. Pharmacother. 5, 1781-1798 (2004).

Platelet Activating Factor CAS Registry Number: 65154-06-5 β-乙酰基-γ-O-烷基-L-α-磷脂酰胆碱

Additional Names: PAF; 1-O-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine; acetyl glyceryl ether phosphorylcholine; AGEPC; PAF-acether; antihypertensive polar renomedullary lipid; APRL
Literature References: Phospholipid mediator of platelet aggregation, inflammation, and anaphylaxis. Produced in response to specific stimuli by a variety of cell types, including neutrophils, basophils, platelets, and endothelial cells. Several molecular species of PAF have been identified which vary in the length of the O-alkyl side chain. In vitro identification of a soluble platelet activating factor produced by antigen stimulated leukocytes: P. M. Henson, J. Exp. Med. 131, 287 (1970). Isoln from rabbit basophils, characterization of PAF response and potential role in immune complex disease: J. Benveniste et al., ibid. 136, 1356 (1972). Isoln from human leukocytes: J. Benveniste, Nature 249, 581 (1974). Release of PAF in vivo during anaphylaxis: R. N. Pinckard et al., J. Immunol. 123, 1847 (1979). Structural study: J. Benveniste et al., Nature 269, 170 (1977); and synthetic approaches: J. Benveniste et al., C.R. Seances Acad. Sci. Ser. D 289, 1037 (1979); C. A. Demopoulos et al., J. Biol. Chem. 254, 9355 (1979). Identity with APRL and antihypertensive activity: M. L. Blank et al., Biochem. Biophys. Res. Commun. 90, 1194 (1979). Structures of 1-O-octadecyl- and 1-O-hexadecyl-PAF, two of the predominant molecular forms: D. J. Hanahan et al., ibid. 255, 5514 (1980). Total synthesis of 1-O-octadecyl-PAF: J. Godfroid et al., FEBS Lett. 116, 161 (1980). Enantiomeric synthesis of C16- and C18-PAF: M. Ohno et al., Chem. Pharm. Bull. 33, 572 (1985). Molecular heterogeneity of naturally occurring PAF: R. N. Pinckard et al., Biochem. Biophys. Res. Commun. 122, 325 (1984); H. W. Mueller et al., J. Biol. Chem. 259, 14554 (1984). Ulcerogenic effects: A.-C. Rosam et al., Nature 319, 54 (1986). Effects on human pulmonary and cardiovascular function: F. M. Cuss et al., Lancet 2, 189 (1986). Review of isoln and analytical methods: D. J. Hanahan, S. T. Weintraub, Methods Biochem. Anal. 31, 195-219 (1985); of chemical and biochemical characteristics: D. J. Hanahan, R. Kumar, Prog. Lipid Res. 26, 1-28 (1987). Reviews of biosynthesis, biological activities and PAF antagonists: P. Braquet et al., Pharmacol. Rev. 39, 97-145 (1987); P. J. Barnes et al., J. Allergy Clin. Immunol. 81, 919-934 (1988). Books: Platelet-Activating Factor and Related Lipid Mediators, F. Snyder, Ed. (Plenum Press, New York, 1987) 471 pp; Prog. Biochem. Pharmacol. 22 entitled "Biologically Active Ether Lipids" by P. Braquet et al., Eds. (Karger, Basel, 1988).

Choline Alfoscerate CAS Registry Number: 28319-77-9 甘油磷酰胆碱

CAS Name: 2-[[[(2R)-2,3-Dihydroxypropoxy]hydroxyphosphinyl]oxy]-N,N,N-trimethylethanaminium hydroxide inner salt
Additional Names: D-choline hydroxide 2,3-dihydroxypropyl hydrogen phosphate inn...
Literature References: Phospholipid; precursor in choline biosynthesis; intermediate in catabolic pathway of phosphatidylcholine. Isoln from bovine pancreas: G. Schmidt et al., J. Biol. Chem. 161, 523 (1945). Synthesis: E. Baer, M. Kates, J. Am. Chem. Soc. 70, 1394 (1948); and properties: N. H. Tattrie et al., Biochem. Prep. 6, 16 (1958). HPLC determn: G. Abbiati et al., J. Chromatogr. 566, 445 (1991). Metabolism and biodistribution: idem et al., Eur. J. Drug Metab. Pharmacokinet. 18, 173 (1993). Clinical pharmacology: N. Canal et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 29, 103 (1991). Clinical pharmacokinetics: G. Gatti et al., ibid. 30, 331 (1992). Clinical study in multi-infarct dementia: L. Frattola et al., Curr. Ther. Res. 49, 683 (1991); in Alzheimer's type dementia: L. Parnetti et al., Drugs Aging 3, 159 (1993).

Phosphocreatine CAS Registry Number: 67-07-2 磷酸肌酸

CAS Name: N-[Imino(phosphonoamino)methyl]-N-methylglycine
Additional Names: N-(phosphonoamidino)sarcosine; creatine phosphate; creatinephosphoric acid; PC
Percent Composition: C 22.76%, H 4....
Literature References: Phosphorylated form of creatine, q.v. Occurs primarily in skeletal muscle; also found in heart and brain. Involved in the transfer of high energy phosphate to ADP. Isoln from frog muscle: Eggleton, Biochem. J. 21, 190 (1927); from cat muscle: Fiske, Subbarow, J. Biol. Chem. 81, 629 (1929). Synthesis by phosphorylation of creatine: Zeile, Fawaz, Z. Physiol. Chem. 256, 193 (1938); Ennor, Stocken, Biochem. J. 43, 190 (1948). Enzymic determn in skeletal muscle: K. Yoshikawa et al., Anal. Biochem. 159, 303 (1986). HPLC determn in cardiac muscle: T. Teerlink et al., Anal. Biochem. 214, 278 (1993). Clinical trial as cardioprotective: M. L. Semenovsky et al., J. Thorac. Cardiovasc. Surg. 94, 762 (1987); as antiarrhythmic: M. Y. Ruda et al., Am. Heart J. 116, 393 (1988). Review of role in energy metabolism: S. P. Bessman, C. L. Carpenter, Annu. Rev. Biochem. 54, 831-862 (1985).

Py-Phe CAS Registry Number: 199612-75-4 4-(1-芘基)丁酰-phe-oh

CAS Name: N-[1-oxo-4-(1-pyrenyl)butyl]-L-phenylalanine
Additional Names: N-(1-phenylalanine)-4-(1-pyrene)butyramide
Percent Composition: C 79.98%, H 5.79%, N 3.22%, O 11.02%
Literature References: Photoactivated chemical protease. Prepn: C. V. Kumar, A. Buranaprapuk, Angew. Chem. Int. Ed. 36, 2085 (1997). Site specificity: idem et al., Proc. Natl. Acad. Sci. USA 95, 10361 (1998).

Platonin CAS Registry Number: 3571-88-8 普拉通宁

CAS Name: 2,2'-[3-[(3-Heptyl-4-methyl-2(3H)-thiazolylidene)ethylidene]-1-propene-1,3-diyl]bis(3-heptyl-4-methylthiazolium) diiodide
Additional Names: 4,4',4''-trimethyl-3,3',3''-triheptyl-8-(2'...
Literature References: Photosensitizing cyanine dye with antimicrobial and immunomodulating activities. General prepn and use in rheumatoid arthritis: I. Yamamoto, BE 894635; idem, US 4464383 (1983, 1984). Antifungal properties: K. Ito, P. K. Kuroda, Bull. Pharm. Res. Inst. Osaka Med. Coll. 3, 20 (1952), C.A. 47, 11335f (1953). Effect on experimentally induced leukopenia: H. Iwata et al., Folia Pharmacol. Jpn. 50, 169 (1954), C.A. 49, 10518b (1955). Immunomodulating effect in animals: H. Ichihashi, T. Kondo, Gann 58, 529 (1967); Y. Oyanagui, Arch. Int. Pharmacodyn. Ther. 266, 162 (1983). Enzyme immunoassay in plasma: I. Yamamoto, K. Morishita, J. Immunoassay 7, 17 (1986). Toxicity study: T. Kimoto, K. Nishitani, Kanko Shikiso 85, 43 (1977), C.A. 86, 84374m (1977).