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

Sincalide CAS Registry Number: 25126-32-3 辛卡利特

CAS Name: 1-De(5-oxo-L-proline)-2-de-L-glutamine-5-L-methioninecaerulein
Additional Names: cholecystokinin C-terminal octapeptide; CCK C-terminal octapeptide; pancreozymin C-terminal octapeptid...
Literature References: The C-terminal octapeptide of cholecystokinin-pancreozymin (see cholecystokinin). Structurally similar to caerulein, q.v., it evokes a variety of biological responses similar to CCK-PZ, including smooth-muscle contraction of the gall bladder and small intestine, relaxation of the choledochoduodenal junction, protein secretion by the pancreas and acid secretion by the stomach. It is more active than cholecystokinin on a weight or molar basis. Initial isoln: V. Mutt, J. E. Jorpes, Eur. J. Biochem. 6, 156 (1968). Prepn: M. A. Ondetti et al., DE 1922185 corresp to US 3723406 (1969, 1970, both to Squibb); eidem, J. Am. Chem. Soc. 92, 195 (1970). Mechanical and metabolic effects: K. E. Andersson et al., Acta Physiol. Scand. 96, 495 (1976). In vitro study: M. Deschodt-Lanckman et al., Gastroenterology 68, 819 (1975). Use in clinical radiology: W. M. Thompson, J. R. Amberg, Gastrointest. Radiol. 3, 191 (1978). Effect on food intake: M. A. Della-Fera, C. A. Baile, Science 206, 471 (1979). Review of synthesis: L. Balaspiri, Acta Physiol. Acad. Sci. Hung. 47, 299 (1976). Review of pharmacology: S. L. Engel et al., in Pharmacological and Biochemical Properties of Drug Substances vol. 2, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1979) pp 516-526.

Dexetimide CAS Registry Number: 21888-98-2 苄替米特

CAS Name: (3S)-3-Phenyl-1'-(phenylmethyl)-[3,4'-bipiperidine]-2,6-dione
Additional Names: (S)-(+)-2-(1-benzyl-4-piperidyl)-2-phenylglutarimide; (+)-3-(1-benzyl-4-piperidyl)-3-phenylpiperidine-2...
Literature References: The dextroenantiomer responsible for the pharmacological activity of racemic benzetimide, q.v. Resolution of isomers and comparative pharmacology: Janssen et al., Arzneim.-Forsch. 21, 1365 (1971). Abs config studies: van Wijngaarden et al., Life Sci. 9, part 1, 1289 (1970); Spek et al., Nature 232, 575 (1971). Clinical trials: De Smedt et al., J. Clin. Pharmacol. 10, 207 (1970).

Borneol CAS Registry Number: 507-70-0 2-茨醇;冰片;龙胆

CAS Name: endo-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol
Additional Names: endo-2-bornanol; endo-2-camphanol; endo-2-hydroxycamphane; bornyl alcohol; Baros camphor; Sumatra camphor; Borneo camph...
Literature References: The dextrorotatory form which predominates occurs in the oil from Dryobalanops aromatica Gaertn., Dipterocarpaceae, and in many other plants; the levorotatory form comes from Blumea balsamifera (L.) DC., Compositae: E. Gildemeister, F. Hoffman, Die ätherischen Ole (Schimmel, Leipzig, 3rd ed., 1928) pp 475-481. Racemic borneol is prepd synthetically by reduction of camphor: Truett, Moulton, J. Am. Chem. Soc. 73, 5913 (1951); Ziegler et al., Ann. 623, 9 (1959); Ziegler, GB 803178 (1958); from pinene: Schwyzer, Pharm. Ztg. 75, 1275 (1930). Configuration (isoborneol = exo-form; borneol = endo-form): Toivonen et al., Acta Chem. Scand. 3, 991 (1949). Toxicity data: R. C. Beier, Rev. Environ. Contam. Toxicol. 113, 47-127 (1990). Review: J. L. Simonsen, The Terpenes vol. II (University Press, Cambridge, 2nd ed., 1949) pp 349-365.

Methylconiine CAS Registry Number: 553-75-3

CAS Name: 1-Methyl-2-propylpiperidine
Percent Composition: C 76.53%, H 13.56%, N 9.92%
Literature References: The d-form is stated to occur in hemlock in small quantities. The l-form can be isolated from residues left in the prepn of coniine by crystn of the hydrobromides. Isoln: Ahrens, Ber. 35, 1330 (1902); Hess, Eichel, ibid. 50, 1386 (1917). Prepns: Leonard, Barthel, J. Am. Chem. Soc. 71, 3098 (1949); Gaumeton, Glacet, Bull. Soc. Chim. Fr. 1959, 1501; Lukes, Cerny, Collect. Czech. Chem. Commun. 24, 1287 (1959); Cervinka, ibid. 26, 673 (1961).

Karaya Gum CAS Registry Number: 9000-36-6 卡拉亚树胶

Additional Names: Gum karaya; kadaya; katilo; kullo; kuteera; sterculia; Indian tragacanth; mucara
Literature References: The dried exudate of the tree Sterculia urens Roxb., Sterculiaceae, found in India, especially in the Gujerat region and in the central provinces: Toothaker, The Soluble Gums (Philadelphia, 1921); Mantell, The Water-Soluble Gums (New York, 1947). Constituents and structure: Hirst, Dunstan, J. Chem. Soc. 1953, 2332. Structure is a partially acetylated polysaccharide containing about 8% acetyl groups and about 37% uronic acid residues. Reviews: F. Smith, R. Montgomery, The Chemistry of Plant Gums and Mucilages (Reinhold, New York, 1959); Goldstein, Alter, in Industrial Gums, R. L. Whistler, Ed. (Academic Press, New York, 2nd ed., 1973) pp 273-287.

Tofisopam CAS Registry Number: 22345-47-7 托非索泮

CAS Name: 1-(3,4-Dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepineTrademarks: Grandaxin (EGYT); Seriel (Biogalenique)
Percent Composition: C 69.09%, H 6.85%, N 7.32%, O 16.7...
Literature References: The first 5H-2,3-benzodiazepine. Prepn: J. Korosi et al., HU 155572 (1969 to Pharm. Res. Inst.), C.A. 70, 115026a (1969); GB 1202579 corresp to US 3736315 (1970, 1973 both to EGYT); J. Korosi, T. Lang, Ber. 107, 3883 (1974). Synthesis and conformation: eidem, Ther. Hung. 23, 132 (1975). FT 13C NMR study: A. Neszmelyi et al., Ber. 107, 3894 (1974). Pharmacology: L. Petocz, I. Kosoczky, Ther. Hung. 23, 134 (1975). Human pharmacokinetics: S. Ronai et al., ibid. 139. Comparative efficacy: H. L. Goldberg, R. J. Finnerty, Am. J. Psychiatry 136, 196 (1979).

Chorismic Acid CAS Registry Number: 617-12-9 分支酸来源于产气肠杆菌

CAS Name: (3R-trans)-3-[(1-Carboxyethenyl)oxy]-4-hydroxy-1,5-cyclohexadiene-1-carboxylic acid
Additional Names: 3-enolpyruvic ether of trans-3,4-dihydroxycyclohexa-1,5-diene carboxylic acid; a-...
Literature References: The first branch point intermediate in the biosynthesis of aromatic amino acids via the shikimate pathway in bacteria, fungi, and higher plants; naturally occurring as the (-)-form. Its existence was predicted, then discovered during development of a mutant of A. aerogenes: M. I. Gibson et al., Nature 195, 1173 (1962); M. I. Gibson, F. Gibson, Biochim. Biophys. Acta 65, 160 (1962). NMR and preliminary structure study: F. Gibson, M. Jackman, Nature 198, 388 (1963). Isoln and metabolism study: M. Gibson, F. Gibson, Biochem. J. 90, 248 (1964). Prepn and characterization of the barium salt: F. Gibson, ibid. 256. Structure, relative and abs config, prepn of the monohydrate: J. M. Edwards, L. M. Jackman, Aust. J. Chem. 18, 1227 (1965). Total synthesis of racemic chorismic acid: D. A. McGowan, G. A. Berchtold, J. Am. Chem. Soc. 104, 1153 (1982); B. Ganem et al., ibid. 6787; improved synthesis: G. A. Berchtold et al., ibid. 105, 6265 (1983); short formal synthesis: G. H. Posner et al., J. Org. Chem. 52, 4836 (1987). Total synthesis of (-)-form: J. L. Pawlak, G. A. Berchtold, ibid. 1765. Potential use in development of herbicides: S. Stinson, Chem. Eng. News 60, 31 (Dec. 6, 1982). Reviews of chorismic acid in biosynthesis of aromatic amino acids: F. Gibson, J. Pittard, Bacteriol. Rev. 32, 465-492 (1968); R. J. Ife et al., J. Chem. Soc. Perkin Trans. 1 1976, 1776-1783; U. Weiss, J. M. Edwards, The Biosynthesis of Organic Compounds (Wiley, New York, 1980) pp 134-143. See also shikimic acid.

Nepetalactone CAS Registry Number: 490-10-8 顺式,反式-荆芥内酯

CAS Name: 5,6,7,7a-Tetrahydro-4,7-dimethylcyclopenta[c]pyran-1-(4aH)-one
Percent Composition: C 72.26%, H 8.49%, O 19.25%
Literature References: The first fully characterized methylcyclopentane monoterpenoid. Isolated from the volatile oil of catnip produced by Nepeta cataria L., Labiatae: S. M. McElvain et al., J. Am. Chem. Soc. 63, 1558 (1941); J. Meinwald, ibid. 76, 4571 (1954). First believed to be a single entity, it was later shown to be a mixture of the cis-trans and trans-cis isomers, the cis-trans isomer comprising 70-99% of the oil. Structure: S. M. McElvain, E. J. Eisenbraun, J. Am. Chem. Soc. 77, 1599 (1955). Configuration of the cis-trans and trans-cis isomers: R. B. Bates et al., ibid. 80, 3420 (1958). Separation and properties: R. B. Bates, C. W. Siegel, Experientia 19, 564 (1963). Biosynthesis: F. E. Regnier et al., Phytochemistry 7, 221 (1968). Metabolism in cats: G. R. Waller et al., Science 164, 1281 (1969). Behavioral and toxicological study: J. W. Harney et al., Lloydia 41, 367 (1978). Structural study of isomeric nepetalactones: E. J. Eisenbraun et al., J. Org. Chem. 45, 3811 (1980).

Vernolepin CAS Registry Number: 18542-37-5 (3aR,4S,5aR,9aR,9bR)-4-羟基-3,9-二亚甲基-5a-乙烯基-3a,4,5,6,9a,9b-六氢吡喃并[5,4-g]苯并呋喃-2,8-苯醌

CAS Name: [3aR-(3aa,4a,5aa,9aa,9bb)]-5a-Ethenyloctahydro-4-hydroxy-3,9-bis(methylene)-2H-furo[2,3-f][2]benzopyran-2,8(3H)-dione
Percent Composition: C 65.21%, H 5.84%, O 28.96%
Literature References: The first recognized naturally occurring elemanolide dilactone; a sesquiterpene lactone with tumor inhibiting properties. Isoln from Vernonia hymenolepsis A. Rich, Compositae and structure: S. M. Kupchan et al., J. Am. Chem. Soc. 90, 3596 (1968); structural elucidation: eidem, J. Org. Chem. 34, 3903 (1969). Biological properties: S. M. Kupchan et al., J. Med. Chem. 14, 1147 (1971). Approach to stereosynthesis of (+)-form: H. Iio et al., Tetrahedron 35, 941 (1979); K. Kondo et al. Tetrahedron Lett. 34, 4219 (1993). Total synthesis of (±)-form: P. A. Grieco et al., J. Am. Chem. Soc. 98, 1612 (1976); F. Zutterman et al., Tetrahedron 35, 2389 (1979).

Myrtol CAS Registry Number: 8002-55-9

Trademarks: Gelomyrtol (Pohl)
Literature References: The fraction of the volatile oil from Myrtus communis L., Myrtaceae distilling between 166-180° and consisting chiefly of eucalyptol and dextro-pinene with a small quantity of an undefined camphor.