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

Alitretinoin CAS Registry Number: 5300-03-8 9-顺式视黄酸

CAS Name: 9-cis-Retinoic acid
Additional Names: 6-cis-retinoic acidTrademarks: Panretin (Ligand)
Percent Composition: C 79.95%, H 9.39%, O 10.65%
Literature References: Naturally occurring derivative of vitamin A, q.v. Morphogenic agent that modulates cell growth and differentiation; activates both retinoic acid (RAR) and retinoid X (RXR) receptors. Prepn: C. D. Robeson et al., J. Am. Chem. Soc. 77, 4111 (1955); M. Matsui et al., J. Vitaminol. 4, 178 (1958); M. F. Boehm et al., J. Med. Chem. 37, 408 (1994). Identification as physiological ligand of RXR: R. A. Heyman et al., Cell 68, 397 (1992); A. A. Levin et al., Nature 355, 359 (1992). Role in morphogenesis: C. Thaller et al., Development 118, 957 (1993). Biosynthesis from all-trans-retinoic acid: J. Urbach, R. R. Rando, Biochem. J. 299, 459 (1994). HPLC determn in plasma: A. M. Dzerk et al., J. Pharm. Biomed. Anal. 16, 1013 (1998). Clinical pharmacokinetics: C. Weber, E. Dumont, J. Clin. Pharmacol. 37, 566 (1997). Clinical evaluation in acute promyelocytic leukemia: S. L. Soignet et al., Leukemia 12, 1518 (1998); in advanced cancers: N. A. Rizvi et al., Clin. Cancer Res. 4, 1437 (1998). Review of role as hormone: B. F. Tate et al., Trends Endocrinol. Metab. 5, 189-194 (1994); of clinical development: J. Cell. Biochem. Suppl. 26, 158-167 (1996).

Acetylcarnitine CAS Registry Number: 3040-38-8; 14992-62-2 ( DL -form) L-乙酰基肉碱

CAS Name: (2R)-2-(Acetyloxy)-3-carboxy-N,N,N-trimethyl-1-propanaminium inner salt
Additional Names: L-(3-carboxy-2-hydroxypropyl)trimethylammonium hydroxide inner salt acetate; acetyl-L-carniti...
Literature References: Naturally occurring ester of carnitine, q.v.; important acetyl donor in metabolic processes. Prepn from carnitine extracted from meat: R. Engeland, Ber. 42, 2457 (1909); R. Krimberg, W. Wittandt, Biochem. Z. 251, 229 (1932); E. Strack et al., Z. Physiol. Chem. 238, 183 (1936). Resolution of isomers: K. Brendel, R. Bressler, Biochim. Biophys. Acta 137, 98 (1967). Extraction from calf brain tissue: E. A. Hosein, A. Orzeck, Int. J. Neuropharmacol. 3, 71 (1964). Enzymatic determn in serum: K. Tomita et al., J. Pharm. Biomed. Anal. 24, 1147 (2001). Clinical trial in cognitive impairment in the elderly: G. Salvioli, M. Neri, Drugs Exp. Clin. Res. 20, 169 (1994). Review of pharmacology in the CNS: L. Janiri, E. Tempesta, Int. J. Clin. Pharmacol. Res. 3, 295-306 (1983); of bioactivity and clinical studies in Alzheimer's disease and geriatric depression: J. W. Pettegrew et al., Mol. Psychiatry 5, 616-632 (2000); of pharmacokinetics and metabolism: C. J. Rebouche, Ann. N.Y. Acad. Sci. 1033, 30-41 (2004).

Diosmin CAS Registry Number: 520-27-4 地奥司明

CAS Name: 7-[[6-O-(6-Deoxy-a-L-mannopyranosyl)-b-D-glucopyranosyl]oxy]-5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-4H-1-benzopyran-4-one
Additional Names: 3',5,7-trihydroxy-4'-methoxyflavone-7-ruti...
Literature References: Naturally occurring flavonic glycoside; rhamnoglycoside of diosmetin, q.v. Isolation from various plant sources: O. A. Oesterle, G. Wander, Helv. Chim. Acta 8, 519 (1925). Elucidation of structure: G. Zemplén, R. Bognár, Ber. 76, 452 (1943). Prepn from hesperidin, q.v.: eidem, ibid.; N. B. Lorette et al., J. Org. Chem. 16, 930 (1951). Isoln from lemon peel (Citrus limon Linn. Rutaceae): R. M. Horowitz, J. Org. Chem. 21, 1184 (1956); from Zanthoxylum avicennae, Rutaceae: H. R. Arthur et al., J. Chem. Soc. 1956, 632; H. R. Arthur et al., ibid. 1959, 4007; from flowers of Sophora microphylla Ait. Leguminosae: L. H. Briggs et al., ibid. 1960, 1955. Toxicology studies: H. Heusser, W. Osswald, Arch. Farmacol. Toxicol. 3, 33 (1977). NMR spectrum: J. L. Nieto, A. M. Gutierrez, Spectrosc. Lett. 19, 427 (1986). Mechanism of action: C. Boudet, L. Peyrin, Arch. Int. Pharmacodyn. 283, 312 (1986). Pharmacology: J. R. Caseley-Smith, J. R. Caseley-Smith, Agents Actions 17, 1 (1985); M. Damon et al., Arzneim.-Forsch. 37, 1149 (1987). HPLC determn in biological fluids: D. Baylocq et al., Ann. Pharm. Fr. 41, 115 (1983). Clinical study in post-phlebitic ulcers: M. C. Nguyen, K. Morere, Gaz. Med. 92, 71 (1985); in acute hemorrhoids: A. Tajana et al., Minerva Med. 79, 387 (1988). Clinical trial in chronic venous insufficiency: R. Laurent et al., Int. Angiol. 7, Suppl. 2, 39 (1988).

Levodopa CAS Registry Number: 59-92-7 左旋多巴

CAS Name: 3-Hydroxy-L-tyrosine
Additional Names: (-)-3-(3,4-dihydroxyphenyl)-L-alanine; L-dopa; b-(3,4-dihydroxyphenyl)-L-alanine; (-)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid
Trademark...
Literature References: Naturally occurring form of dopa, q.v., the biological precursor of the catecholamines. Prepn from l-3-nitrotyrosin: Wasser, Lewandowski, Helv. Chim. Acta 4, 657 (1921); from 3-(3,4-methylenedioxyphenyl)-L-alanine: Yamada et al., Chem. Pharm. Bull. 10, 693 (1962); from L-tyrosine: Vorbrüggen, Krolikiewicz, Ber. 105, 1168 (1972); Bretschneider et al., Helv. Chim. Acta 56, 2857 (1973); from Vicia faba beans: Wysong, US 3253023 (1966 to Dow Chem.); by fermentation of L-tyrosine: Sih et al., J. Am. Chem. Soc. 91, 6204 (1969); Florent, Renaut, DE 2102793 (1971 to Rhône-Poulenc), C.A. 75, 108505f (1971). Sepn from racemate: Vogler, Baumgartner, Helv. Chim. Acta 35, 1776 (1952); NL 6514950; US 3405159 (1966, 1968 both to Merck Co.). Molecular conformation: Becker et al., Biochem. Biophys. Res. Commun. 41, 444 (1970). Metabolism studies: Shaw et al., J. Biol. Chem. 226, 255 (1957); Calne et al., Br. J. Pharmacol. 37, 57 (1969). Hemodynamic effects in congestive heart failure: S. I. Rajfer et al., N. Engl. J. Med. 310, 1357 (1984). Series of articles on clinical efficacy in Parkinson's disease: Adv. Neurol. 45, 457-510 (1986). Reviews on L-dopa and parkinsonism: Barbeau, Can. Med. Assoc. J. 101, 791 (1969); Pletscher et al., Schweiz. Med. Wochenschr. 100, 797 (1970); Calne, Sandler, Nature 226, 21 (1970); L-Dopa and Parkinsonism, A. Barbeau, Ed. (F. A. Davis, Philadelphia, 1970). Review of acute toxicity data: W. G. Clark et al., Toxicol. Appl. Pharmacol. 28, 1-7 (1974). Comprehensive description: R. Gomez et al., Anal. Profiles Drug Subs. 5, 189-223 (1976).

Hypusine CAS Registry Number: 34994-11-1 (2S)-2-氨基-6-[[(2S)-4-氨基-2-羟基丁基]氨基]己酸

CAS Name: N6-[(2R)-4-Amino-2-hydroxybutyl]-L-lysine
Additional Names: (2S,9R)-2,11-diamino-9-hydroxy-7-azaundecanoic acid; N6-(4-amino-2-hydroxybutyl)-2,6-diaminohexanoic acid
Percent Compos...
Literature References: Naturally occurring L-amino acid formed by the post-translational modification of lysine. Name coined to indicate the condensation product of hydroxyputrescine with lysine. Isoln: T. Shiba et al., Biochim. Biophys. Acta 244, 523 (1971); from archaebacteria: H. Schümann, F. Klink, Syst. Appl. Microbiol. 11, 103 (1989). In eukaryotes occurs only at a single position in one protein, eukaryotic protein synthesis initiation factor 5A, (eIF-5A, formerly eIF-4D): M. H. Park et al., Proc. Natl. Acad. Sci. USA 78, 2869 (1981); H. L. Cooper et al., ibid. 80, 1854 (1983). Biosynthesis: M. H. Park et al., J. Biol. Chem. 257, 7217 (1982); M. H. Park et al., ibid. 259, 12123 (1984). Synthesis and stereochemistry: T. Shiba et al., Bull. Chem. Soc. Jpn. 55, 899 (1982). Total synthesis: C. M. Tice, B. Ganem, J. Org. Chem. 48, 5043, 5048 (1983); R. J. Bergeron et al., ibid. 58, 6804 (1993). Biological significance in eukaryotes: J. W. B. Hershey et al., Biochim. Biophys. Acta 1050, 160 (1990). HPLC determn in eukaryotic samples: S. Beninati et al., Anal. Biochem. 184, 16 (1990). Chromatographic determn in archaebacteria: D. Bartig, F. Klink, J. Chromatogr. 606, 43 (1992). Review of biological significance: M. H. Park et al., Trends Biochem. Sci. 18, 475-479 (1993).

Lupinine CAS Registry Number: 486-70-4 ((1R,9aR)-八氢-1H-喹嗪-1-基)甲醇

CAS Name: [1R-trans]-Octahydro-2H-quinolizine-1-methanol
Additional Names: l-lupinine; (-)-lupinine
Percent Composition: C 70.96%, H 11.31%, N 8.28%, O 9.45%
Literature References: Naturally occurring l-form isolated from seeds and herb of Lupinus luteus L. and other L. species, Leguminosae also found in Anabasis aphylla L., Chenopodiaceae. Extraction procedure: J. F. Couch, J. Am. Chem. Soc. 56, 2434 (1934). Structure and synthesis: R. W. Willstätter, E. Fourneau, Ber. 35, 1910 (1902); P. Karrer et al., Helv. Chim. Acta 11, 1062 (1928); K. Winterfeld, F. W. Holschneider, Ber. 64B, 137, 692 (1931); K. Winterfeld, ibid. 692. Synthesis of racemic lupinine: F. W. Holschneider, K. Winterfeld, Arch. Pharm. 277, 192 (1939); G. C. Gerrans et al., Tetrahedron Lett. 1975, 4171; T. Iwashita et al., J. Org. Chem. 47, 230 (1982). Synthesis of racemic lupinine and epi-lupinine: G. R. Clemo et al., J. Chem. Soc. 1937, 965; H. Takahata et al., Chem. Pharm. Bull. 34, 4523 (1986); of l-epi-lupinine: M. L. Bremmer, S. M. Weinreb, Tetrahedron Lett. 24, 261 (1983). Absolute configuration of (-)-form: R. C. Cookson, Chem. Ind. (London) 1953, 339. Crystal structure: A. Koziol et al., Acta Crystallogr. B34, 3491 (1978). Biosynthesis: Soucek, Schutte, Angew. Chem. 74, 901 (1962); W. M. Golebiewski, I. D. Spenser, J. Am. Chem. Soc. 106, 1441 (1984).

Asarinin CAS Registry Number: 133-04-0 细辛脂素

CAS Name: [1R-(1a,3aa,4b,6aa)]-5,5'-(Tetrahydro-1H,3H-furo[3,4-c]furan-1,4-diyl)bis-1,3-benzodioxole
Additional Names: l-asarinin; (-)-episesamin; xanthoxylin S
Percent Composition: C 67.79%...
Literature References: Naturally occurring l-form isolated from Xanthoxylum clava-herculis L. (X. carolinianum Lam.), Rutaceae; Asarum sieboldi Miguel var. seulensis Nakai, A. blumei Duch., Aristolochiaceae: Colton, Am. J. Pharm. 52, 191 (1880); Eberhardt, ibid. 62, 231 (1890); Gordin, J. Am. Chem. Soc. 28, 1649 (1906); H. Dieterle et al., Arch. Pharm. 269, 384 (1931); Huang-Minlon, Ber. 70, 951 (1937); T. Kaku et al., Keijo J. Med. 9, 1 (1934); C.A. 32, 90901 (1938). Structure: H. Dieterle, K. Schwenger, Arch. Pharm. 277, 33 (1939). Synthesis of dl-form: M. Beroza, M. S. Schechter, J. Am. Chem. Soc. 78, 1242 (1956); K. Freudenberg, E. Fischer, Ber. 89, 1230 (1956); D. R. Stevens, D. A. Whiting, Tetrahedron Lett. 27, 4629 (1986). Diastereoisomeric with sesamin, q.v. Stereochemistry of the d-form: K. Freudenberg, G. S. Sidhu, ibid. 94, 851 (1961). Antitubercular activity: Ramaswamy, Naturwissenschaften 44, 380 (1957).

Monobutyrin CAS Registry Number: 557-25-5 丁酸甘油酯

CAS Name: Butanoic acid 2,3-dihydroxypropyl ester
Additional Names: 1-butyrylglycerol; a-monobutyrin; glycerol a-monobutyrate; glyceryl 3-monobutyrate
Percent Composition: C 51.84%, H 8.70%,...
Literature References: Naturally occurring lipid that stimulates angiogenesis. Secreted by differentiating adipocytes; stimulates blood vessel formation and causes vasodilation. The (R)-isomer is bioactive. Prepn of optical isomers: E. Abderhalden, E. Eichwald, Ber. 48, 1847 (1915); of L-form: E. Baer, H. O. L. Fischer, J. Am. Chem. Soc. 67, 2031 (1945); S. Gronowitz et al., Chem. Phys. Lipids 14, 174 (1975). Purification from adipocytes and identification of angiogenic activity: D. E. Dobson et al., Cell 61, 223 (1990). Biosynthesis: W. O. Wilkison et al., J. Biol. Chem. 266, 16886 (1991); W. O. Wilkison, B. M. Spiegelman, ibid. 268, 2844 (1993). Effect on retinal circulation and probable role in pathology of diabetes: Y.-D. C. Halvorsen et al., J. Clin. Invest. 92, 2872 (1993).

Pregnan-3 a -ol-20-one CAS Registry Number: 128-20-1 孕烷醇酮

CAS Name: (3a,5b)-3-Hydroxypregnan-20-one
Additional Names: 3a-hydroxy-5b-pregnan-20-one; pregnanolone; eltanolonePercent Composition: C 79.19%, H 10.76%, O 10.05%
Literature References: Naturally occurring metabolite of progesterone, q.v. Isoln from urine of pregnant women: R. E. Marker, O. Kamm, J. Am. Chem. Soc. 59, 1373 (1937); from bile of pregnant cows: W. H. Pearlman, E. Cerceo, J. Biol. Chem. 176, 847 (1948). Prepn: R. E. Marker et al., J. Am. Chem. Soc. 59, 1841 (1937); L. Gyermek et al., J. Med. Chem. 11, 117 (1968); T. L. G. Lemos, J. D. McChesney, J. Nat. Prod. 53, 152 (1990). Pharmacokinetics and pharmacodynamics: P. Carl et al., Acta Anaesthesiol. Scand. 38, 734 (1994). Comparative clinical evaluation: J. Van Hemelrijck et al., Anesthesiology 80, 36 (1994); H. Eriksson et al., Acta Anaesthesiol. Scand. 39, 479 (1995). Hemodynamic effects in humans: J. W. Sear et al., J. Clin. Anesth. 7, 126 (1995).

Allopregnan-3 a -ol-20-one CAS Registry Number: 516-54-1 5alpha-孕甾-3alpha-醇-20-酮

CAS Name: 3a-Hydroxy-5a-pregnan-20-one
Additional Names: 5a-pregnan-3a-ol-20-one; epiallopregnanolone; allotetrahydroprogesterone
Percent Composition: C 79.19%, H 10.76%, O 10.05%
Literature References: Naturally occurring metabolite of progesterone. Prototype of the neuroactive steroids known as epalons that allosterically modulate g-aminobutyric acid type A (GABAA) receptors in the CNS. Isoln from human pregnancy urine: R. E. Marker et al., J. Am. Chem. Soc. 59, 616 (1937). Prepn from pregnenolone: G. Fleischer et al., ibid. 60, 79 (1938). Chromatographic determn in urine: F. J. Bègue et al., J. Chromatogr. Sci. 12, 763 (1974). Synthesis, metabolism and pharmacology: R. H. Purdy et al., J. Med. Chem. 33, 1572 (1990). Review of pharmacology and therapeutic potential of epalons: K. W. Gee et al., Crit. Rev. Neurobiol. 9, 207-227 (1995).