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

Arogenic Acid CAS Registry Number: 53078-86-7

CAS Name: [1(S)-cis]-a-Amino-1-carboxy-4-hydroxy-2,5-cyclohexadiene-1-propanoic acid
Additional Names: L-(8S)-b-(1-carboxy-4-hydroxy-2,5-cyclohexadien-1-yl)alanine; arogenate; pretyrosine
Pe...
Literature References: Precursor in the biosynthesis of L-phenylalanine and L-tyrosine, distributed widely in nature. Pseudomonad bacteria and plants use both the prephenate and arogenate pathways for L-tyrosine biosynthesis. In cyanobacteria, coryniform bacteria and at least one yeast organism the arogenate pathway has been identified as the sole route of L-tyrosine biosynthesis. Identification of arogenate (pretyrosine) in blue-green algae biosynthesis of L-tyrosine: S. L. Stenmark et al., Nature 247, 290 (1974). Dual enzymic routes to L-tyrosine and L-phenylalanine via arogenate (pretyrosine) in P. aeruginosa: N. Patel et al., J. Biol. Chem. 252, 5839 (1977). Isoln and prepn: R. A. Jensen et al., J. Bacteriol. 132, 896 (1977). Confirmation that arogenate is an obligatory intermediate of L-tyrosine biosynthesis: A. M. Fazel et al., Proc. Natl. Acad. Sci. USA 77, 1270 (1980). Structure and config: L. O. Zamir et al., J. Am. Chem. Soc. 102, 4499 (1980). Synthesis via immobilized microbial proteins: eidem, Bioorg. Chem. 11, 32 (1982). Arogenate pathway of tyrosine and phenylalanine biosynthesis in P. aureofaciens: B. Keller et al., J. Gen. Microbiol. 128, 1199 (1982).

Podophyllotoxin CAS Registry Number: 518-28-5 鬼臼毒素

CAS Name: (5R,5aR,8aR,9R)-5,8,8a,9-Tetrahydro-9-hydroxy-5-(3,4,5-trimethoxyphenyl)furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
Additional Names: 1-hydroxy-2-hydroxymethyl-6,7-methylenedi...
Literature References: Precursor of antineoplastics etoposide, teniposide, q.q.v. Found in the rhizomes of North American Podophyllum peltatum L., Podophyllaceae: V. Podwyssotski, Arch. Exp. Pathol. Pharmakol. 13, 29 (1880); also in P. emodi Wall.: von Wartburg et al., Helv. Chim. Acta 40, 1331 (1957); in Juniperus virginiana L., Cupressaceae: Kupchan et al., J. Pharm. Sci. 54, 659 (1965). Structure and absolute configuration: Schrecker, Hartwell, J. Org. Chem. 21, 381 (1956). Crystal structure: T. J. Petcher et al., J. Chem. Soc. Perkin Trans. 2 1973, 288. Synthesis: Gensler, Gatsonis, J. Am. Chem. Soc. 84, 1748 (1962); T. Kaneko, H. Wong, Tetrahedron Lett. 28, 517 (1987). Asymmetric total synthesis: R. C. Andrews et al., J. Am. Chem. Soc. 110, 7854 (1988); E. J. Bush, D. W. Jones, Chem. Commun. 1993, 1200. Toxicity data: F. S. Phillips et al., Fed. Proc. 7, 249 (1948). ELISA determn in plants: K.-J. Yoo, J. R. Porter, J. Nat. Prod. 56, 715 (1993). Clinical evaluation for treatment of genital warts: A. Lassus, Lancet 2, 513 (1987); K. R. Beutner et al., ibid. 1, 831 (1989). Review of early literature: Hartwell, Schrecker in Fortschr. Chem. Org. Naturst. 15, 98-121 (1958). Review of chemistry and antineoplastic activity: I. Jardine, Anticancer Agents Based on Natural Product Models, J. M. Cassady, J. D. Douros, Eds. (Academic Press, New York, 1980) pp 319-351. Review of syntheses: R. S. Ward, Synthesis 1992, 719-730. Review: D. L. Sackett, Pharmacol. Ther. 59, 163-228 (1993).

Biliverdine CAS Registry Number: 114-25-0 去氫膽紅素

CAS Name: 3,18-Diethenyl-1,19,22,24-tetrahydro-2,7,13,17-tetramethyl-1,19-dioxo-21H-biline-8,12-dipropanoic acid
Additional Names: 1,19,22,24-tetrahydro-2,7,13,17-tetramethyl-1,19-dioxo-3,18-di...
Literature References: Precursor of bilirubin. Formed in the body from hemoglobin. The bile of amphibia and of birds contains biliverdine only. Does not occur in normal human bile or normal human serum, but regularly accompanies bilirubin in the serum of patients with carcinomatous obstruction of the bile duct, and frequently in that of patients with liver cirrhosis, catarrhal jaundice, and bile duct occlusion by gallstones. Can be obtained by autooxidation of bilirubin in alkaline soln but the yield is poor: Lemberg, Biochem. J. 28, 978 (1934); better yields by oxidation of bilirubin with ferric chloride in glacial acetic acid: Lemberg, Ann. 499, 25 (1932); by coupled oxidation of hemoglobin and ascorbic acid: Lemberg et al., Biochem. J. 35, 363 (1941); by oxidation of bilirubin with ferric chloride in methanol: Gray et al., J. Chem. Soc. 1961, 2264. Crystal and molecular structure: W. S. Sheldrick, J. Chem. Soc. Perkin Trans. 2 1976, 1457. Comprehensive reviews: Lemberg, Legge, Hematin Compounds and Bile Pigments (New York, 1949); With, Bile Pigments (Academic Press, New York, 1968).

Reticuline CAS Registry Number: 485-19-8 牛心果鹼

CAS Name: 1,2,3,4-Tetrahydro-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methyl-7-isoquinolinol
Additional Names: 1,2,3,4-tetrahydro-6-methoxy-2-methyl-1-vanillyl-7-isoquinolinol; 2-methy...
Literature References: Precursor of many aporphine and morphine-type alkaloids. Isoln of d-form from Anona reticulata Linn., Anonaceae: Gopinath et al., Ber. 92, 776 (1959); dl-form from opium: Brochmann-Hanssen, Furuya, J. Pharm. Sci. 53, 575 (1964); Planta Med. 12, 328 (1964). Structure: Brochmann-Hanssen, Nielson, Tetrahedron Lett. 1965, 1271. Configuration: Battersby, Evans, ibid. 1275. Synthesis of amorphous dl-form: Gopinath et al., Ber. 92, 1657 (1959); P. Kerekes et al., Acta Chim. Acad. Sci. Hung. 98, 491 (1978). Synthesis of crystalline dl-form: Baxter et al., J. Chem. Soc. C 1965, 3645; Chan, Maitland, ibid. 1966, 753; K. C. Rice, A. Brossi, J. Org. Chem. 45, 592 (1980); G. Dornyei et al., Tetrahedron Lett. 1982, 2913. Asymmetric synthesis of (S)-reticuline: Konda et al., Chem. Pharm. Bull. 23, 1063 (1975). Biosynthesis: D. S. Dewan et al., J. Chem. Soc. Perkin Trans. 1 1977, 1662; A. Barrett et al., ibid. 1979, 652.

Chanoclavine CAS Registry Number: 2390-99-0 裸麦角碱

CAS Name: [4R-[4a,5b(E)]]-2-Methyl-3-[1,3,4,5-tetrahydro-4-(methylamino)benz[cd]indol-5-yl]-2-propen-1-ol
Additional Names: (E)-8,9-didehydro-6-methyl-6,7-secoergoline-8-methanol; chanoclavin-I...
Literature References: Precursor of the tetracyclic ergolines, agroclavine, elymoclavine, and lysergic acid amide, q.q.v.: Gröger et al., Z. Naturforsch. 21b, 827 (1966); Floss et al., Chem. Commun. 1967, 105. Occurs in sclerotia of Claviceps purpurea (Fries) Tul., Hypocreaceae, in Ipomea tricolor Cav., Convolvulaceae and is one of the active principles of the ancient Aztec drug "Ololiuqui," Rivea coryrubosa (L.) Hall. f., Convolvulaceae: Hofmann, Tscherter, Experientia 16, 414 (1960). Isoln and structure: Hofmann et al., Helv. Chim. Acta 40, 1358 (1957). Isoln of stereoisomers: Stauffacher, Tscherter, ibid. 47, 2186 (1964). Stereochemistry: Acklin et al., Chem. Commun. 1966, 799. Biosynthetic studies: Floss et al., J. Am. Chem. Soc. 90, 6500 (1968). Total synthesis of (±)-chanoclavine: H. Plieninger et al., Tetrahedron Lett. 1975, 1827; H. Plieninger, D. Schmalz, Ber. 109, 2140 (1976); M. Natsume, H. Muratake, Heterocycles 16, 375 (1981).

Catharanthine CAS Registry Number: 2468-21-5 长春质碱

CAS Name: 3,4-Didehydroibogamine-18-carboxylic acid methyl ester
Additional Names: 7-ethyl-9,10,12,13-tetrahydro-6,9-methano-5H-pyrido[1',2':1,2]azepino[4,5-b]indole-6(6aH)-carboxylic acid meth...
Literature References: Precursor of vinblastine-type alkaloids. Isoln from Vinca rosea Linn. (Catharanthus roseus G. Don.) Apocynaceae: M. Gorman et al., J. Am. Pharm. Assoc. Sci. Ed. 48, 256 (1959); G. H. Svoboda et al., ibid. 659. Structure: N. Neuss, M. Gorman, Tetrahedron Lett. 1961, 206. Abs config: K. Bláha et al., ibid. 1972, 2763. Synthesis of (±)-form: A. A. Qureshi, A. I. Scott, Chem. Commun. 1968, 947, 948; A. R. Battersby et al., ibid. 951; G. Büchi et al., J. Am. Chem. Soc. 92, 999 (1970); J. P. Kutney, F. Bylsma, Helv. Chim. Acta 58, 1672 (1975); B. M. Trost et al., J. Org. Chem. 44, 2052 (1979); T. Imanishi et al., Tetrahedron Lett. 21, 3285 (1980).

Prednimustine CAS Registry Number: 29069-24-7 泼尼莫司汀

CAS Name: (11b)-21-[4-[4-[Bis(2-chloroethyl)amino]phenyl]-1-oxobutoxy]-11,17-dihydroxypregna-1,4-diene-3,20-dione
Additional Names: 11b,17,21-trihydroxypregna-1,4-diene-3,20-dione 21-[4-[p-[bis...
Literature References: Prednisolone ester of chlorambucil, q.v. Prepn: H. F. Fex et al., DE 2001305 corresp to US 3732260 (1970, 1973 both to AB Leo). In vitro study: A. H. Evenaar et al., Eur. J. Cancer 9, 773 (1973). Metabolism: R. Y. Kirdani et al., Oncology 35, 47 (1978). Clinical studies: L. Hakarsson et al., ibid. 103; J. E. Johnsson et al., Cancer Treat. Rep. 63, 421 (1970). Toxicity and antitumor activity study: K. R. Harrap et al., Eur. J. Cancer 13, 873 (1977). Series of articles on pharmacology, toxicology and clinical efficacy: Semin. Oncol. 13, Suppl. 1, 1-44 (1986).

Pendimethalin CAS Registry Number: 40487-42-1 二甲戊灵

CAS Name: N-(1-Ethylpropyl)-3,4-dimethyl-2,6-dinitrobenzenamine
Additional Names: N-(1-ethylpropyl)-2,6-dinitro-3,4-xylidine; N-(1-ethylpropyl)-3,4-dimethyl-2,6-dinitroaniline; penoxalinTradema...
Literature References: Pre-emergence and pre-planting herbicide. Prepn: R. H. Kupelian, DE 2232263 C.A. 78, 84010z (1973) and A. W. Lutz, R. E. Diehl, DE 2241408 C.A. 78, 135858s (1973) (both 1973 to Am. Cyanamid). Activity: H. A. Roberts, W. Bond, Proc. 12th Br. Weed Control Conf. 1, 387 (1974). Persistence in soil: A. Walker, W. Bond, Pestic. Sci. 8, 359 (1977).

Cinmethylin CAS Registry Number: 87818-31-3 环庚草醚

CAS Name: exo-(±)-1-Methyl-4-(1-methylethyl)-2-[(2-methylphenyl)methoxy]-7-oxabicyclo[2.2.1]heptane
Additional Names: (±)-2-exo-(2-methylbenzyloxy)-1-methyl-4-isopropyl-7-oxabicyclo[2...
Literature References: Pre-emergence grass herbicide. Member of the cineole eucalyptol, q.v., family. Prepn: G. B. Payne et al., EP 81893 (1983 to Shell); eidem, US 4670041 (1987 to Du Pont). Physical and chemical properties: B. T. Grayson et al., Pestic. Sci. 21, 143 (1987). Mechanism of action study: M. H. El-Deek, F. D. Hess, Weed Sci. 34, 684 (1986). Metabolism in rats: P. W. Lee et al., J. Agric. Food Chem. 34, 162 (1986). Mobility in soil: D. R. Wendt et al., Proc. South. Weed Sci. Soc. 1987, 391; and herbicidal activity: P. C. Lolas, A. Galopoulos, Zizaniology 1, 221 (1985). Field studies in tobacco: P. C. Lolas, Proc. Br. Crop Prot. Conf. - Weeds 1985, 841; in soybeans: P. C. Bhowmik, Weed Sci. 36, 678 (1988).

Dimethenamid CAS Registry Number: 87674-68-8 二甲吩草胺

CAS Name: 2-Chloro-N-(2,4-dimethyl-3-thienyl)-N-(2-methoxy-1-methylethyl)acetamideTrademarks: Frontier (BASF); Guardsman (BASF)
Percent Composition: C 52.26%, H 6.58%, Cl 12.86%, N 5.08%, O 11....
Literature References: Preemergence herbicide for use in food crops. Prepn: K. Seckinger et al., GB 2114566; eidem, US 4666502 (1983, 1987 both to Sandoz). Bioactivity of stereoisomers: M. Couderchet et al., Pestic. Sci. 50, 221 (1997). Comprehensive description: J. Harr et al., Proc. Br. Crop Prot. Conf. - Weeds 1991, 87-92. Review of field trials and persistence in soil: A. Rahman, T. K. James, Proc. 45th N. Z. Plant Prot. Conf. 1992, 84-88.