CAS: 13429-83-9; (1S,4R)-4,7,7-Trimethyl-3-Oxo-2-Oxabicyclo[2.2.1]Heptane-1-Carboxylic Acid

相似化合物

67111-66-4 39637-74-6 54200-37-2

上下游产品

1-Bromo-5,8,8-trimethyl-3-oxa-bicyclo[3.2.1]°Ctane-2,4-dione hept-5-en-2-endo-yl(1S)-camphanate(1R,2R,4R)-2-exo-cyano-7-oxabicyclo2.2.1hept-5-en-2-endo-yl(1S)-camphanate (-)-(1R,3R)-3-chlor°Camphoric anhydride (1S)-(-)-camphanic chloride (R)-Methoxy-phenyl-acetic acid (4bR,8aR,9R)-7-[1-ethoxycarbonyl-meth-(E)-ylidene]-2-methoxy-4b,5,6,7,8,8a,9,10-°Ctahydro-phenanthren-9-yl ester -3,5'-O-dibenzylpyridoxamine4'-N-camphanyl-(4'R)-4-2H1-3,5'-O-dibenzylpyridoxamine -3,5'-O-dibenzylpyridoxamine4'-N-camphanyl-(4'S)-4-2H1-3,5'-O-dibenzylpyridoxamine -3,5'-O-dibenzylpyridox-4'-yl camphanate(4'R)-4'-2H1-3,5'-O-dibenzylpyridox-4'-yl camphanate

D-樟脑酸置于五氯化磷,三氯氧磷,硫酸体系中,用 水 用作溶剂,化学反应 17.0H,以40%的收率获得(1S)-(-)-樟脑烷酸
参考文献:Pgi 2激动剂的实用合成:手性中间体的拆分-反转-回收方法
标题:Pgi 2激动剂的实用合成:手性中间体的拆分-反转-回收方法
摘要:实用合成((2 R)-5-苄氧基-2-羟基-1,2,3,4-四氢萘-2-基)甲醇((R)-7B),这是合成该新型手性化合物的关键手性中间体通过非对映选择性结晶的光学拆分获得pgi 2激动剂(R)-[6-[(二苯基氨基甲酰氧基)甲基]-6-羟基-5,6,7,8-四氢萘-1-基氧基]乙酸(1).的酯衍生物18外消旋的(5-苄氧基-2-羟基-1,2,3,4-四氢萘-2-基)甲醇(的图7B)与(1小号,4-[r )-(-)-莰烷酸(( −)-Cpoh),然后进行皂化.从可商购获得的5-羟基-1-四氢萘酮(2)开始,此过程的特点是通过酸催化环氧化物衍生物(S)-11水解c2羟基而使不需要的对映异构体(S)-7B再循环.进行这种拆分-反转-再循环方法,得到了外消旋7B的(R)-7B(> 99%ee)的总产率为44%.然后将通过这种方法合成的对映纯(R)-7B用于制备1.这种强大,可重现和可扩展的1合成
Doi:10.1021/op3003085

专利信息

专利号:WO-9804535-A1
优先权日:1996-07-26
标 题 :A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors
发明人：PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA
权利人:DU PONT MERCK PHARMA
摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of formula (VI-a) is particularly effective in the treatment of HIV.

专利号:US-6348616-B1
优先权日:1996-07-26
标题 :Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors
发明人：PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA
摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of the formula:is particularly effective in the treatment of HIV.

专利号:US-5932726-A
优先权日:1996-12-16
标 题 :Asymmetric synthesis of benzoxazinones
发明人：PIERCE MICHAEL ERNEST; CHOUDHURY ANUSUYA; PARSONS JR RODNEY LAWRENCE; RADESCA LILIAN ALICIA
权利人:DU PONT PHARM CO
摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-6040480-A
优先权日:1997-04-07
标题 :Asymmetric synthesis of benzoxazinones
发明人：PIERCE MICHAEL E; CHEN CHENG Y; CHOUDHURY ANUSUYA; RADESCA LILIAN A; TAN LUSHI; ZHAO DALIAN
权利人:DU PONT PHARM CO
摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

专利号:US-5322944-A
优先权日:1991-07-01
标 题:Process for the synthesis of enantiomers of 3-aminochroman compounds
发明人：GUILLAUMET GERALD; FUGIER CLAUDE; SOUVIE JEAN-CLAUDE J; ADAM GERARD; RENARD PIERRE; CAIGNARD DANIEL-HENRI
权利人:ADIR
摘要:Process for preparing enantiomers of general formula (I): ##STR1## where Z, R 1 , R 2 , R 3 and n are defined in the description. The compounds obtained according to the invention are useful as medicinal products.

专利号:US-5112972-A
优先权日:1989-06-02
标 题 :Synthesis of chroman derivatives
发明人：GERICKE ROLF; BAUMGARTH MANFRED; LUES INGEBORG; BERGMANN ROLF; PEYER DE
权利人:MERCK PATENT GMBH
摘要:The invention relates to new chroman derivatives of the formula I in which R1 is A, R2 and R8 are each H or A, R1 and R2 together are also alkylene with 3-6 C atoms, R3 is OH, OA or OAc, R4 is H, R3 and R4 together are also a bond, R5 is Ar or CnH2n-R9, R9 is alkenyl or alkynyl with 2-4 C atoms in each case, OH, OA, CHO, CO-A, CS-A, COOH, COOA, COO-alkyl-Ar, CS-OA, NO2, NH2, NHA, NA2, CN, F, Cl, Br, I, CF3, SA, SO-A, SO2-A or Ar, Ar is a phenyl group which is unsubstituted or substituted once or twice by R10, R6, R7 and R10 are each H, A, HO, AO, CHO, ACO, CF3CO, ACS, HOOC, AOOC, AO-CS, ACOO, A-CS-O, hydroxy-alkyl, mercapto-alkyl, NO2, NH2, NHA, NA2, CN, F, Cl, Br, I, CF3, AS, ASO, ASO2, AO-SO, AO-SO2, AcNH, AO-CO-NH, H2NSO, HANSO, A2NSO, H2NSO2, HANSO2, A2NSO2, H2NCO, HANCO, A2NCO, H2NCS, HANCS, A2NCS, ASONH, ASO2NH, AOSONH, AOSO2NH, ACO-alkyl, nitro-alkyl, cyano-alkyl, A-C(=NOH), A-C(=NNH2), H2PO3 or A2PO3, n is 1, 2 or 3, A is alkyl with 1-6 C atoms, -alkyl is alkylene with 1-6 C atoms and AC is alkanoyl with 1-8 C atoms or aroyl with 7-11 C atoms, and the salts thereof which display effects on the cardiovascular system and can be used for the treatment or prophylaxis of heart failure, angina pectoris, high blood pressure, incontinence and alopecia.