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1. 发明授权

US3976689A Process for preparing 3-fluoro-D-alanine and its deutero analogs 失效
标题翻译：制备3-氟-D-丙氨酸及其氘代类似物的方法
公开(公告)号：US3976689A
公开(公告)日：1976-08-24
申请号：US525708
申请日：1974-11-20
申请人： Donald F. Reinhold
发明人： Donald F. Reinhold
IPC分类号： C07C5/00 , C07C99/00 , C07C101/10
CPC分类号： C07C227/08 , C07B53/00 , C07B59/001 , C07B2200/05
摘要： 3-Fluoro-D-alanine and its deutero analogs, which are potent antibacterial agents, are prepared from fluoropyruvic acid by asymmetric synthesis using an optically active amine such as D-.alpha.-methyl-benzylamine.
摘要翻译：作为有效的抗菌剂的3-氟-D-丙氨酸及其氘代类似物通过使用光学活性胺如D-α-甲基 - 苄胺的不对称合成由氟代丙酸制备。

2. 发明授权

US4220775A Preparation of 4-aza-17-substituted-5.alpha.-androstan-3-ones useful as 5.alpha.-reductase inhibitors 失效
标题翻译：可用作5α-还原酶抑制剂的4-氮杂-17-取代-5α-雄甾烷-3-酮的制备
公开(公告)号：US4220775A
公开(公告)日：1980-09-02
申请号：US20372
申请日：1979-03-15
申请人： Gary H. Rasmusson , David B. R. Johnston , Donald F. Reinhold , Torleif Utne , Ronald B. Jobson
发明人： Gary H. Rasmusson , David B. R. Johnston , Donald F. Reinhold , Torleif Utne , Ronald B. Jobson
IPC分类号： C07C62/24 , C07J1/00 , C07J3/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J73/00 , C07D221/18
CPC分类号： C07J43/003 , C07C62/24 , C07J1/0022 , C07J21/00 , C07J3/005 , C07J33/007 , C07J41/0016 , C07J41/0066 , C07J73/005 , C07C2103/16 , Y10S514/859
摘要： A method of preparing a compound of the formula: ##STR1## where Formula (I) may also have the structure of partial Formula (III); wherein, ##STR2## R' is hydrogen or methyl; R" is hydrogen or .beta.-methyl;R'" is .beta.-methyl or hydroxy;Z is (1) oxo;(2) .beta.-hydrogen and .alpha.-hydroxy; or .alpha.-hydrogen or .alpha.-hydroxyl and(3) (Y).sub.n Q where n=0 or 1, Y is a straight or branched hydrocarbon chain of 1 to 12 carbon atoms andQ is ##STR3## where R.sup.8 is, ##STR4## where the dashed bond replaces the 17.alpha. hydrogen; (6) cyano; or(7) tetrazolyl;and pharmaceutically acceptable salts of the above compounds;CHARACTERIZED IN THAT(I.) a compound of the formula: ##STR5## , where A has the meanings above except --CH.dbd.CH--, is (1) treated with an oxidizing agent at reduced temperatures to form the corresponding 5-oxo-3,5-seco-androstan-3-oic acid compound;(2) treating the product of step (1) with an amine of formula: R.sup.1 NH.sub.2 to form the corresponding 4-aza-5-androsten-3-one compound substituted in the 4-position with R.sup.1 ; and(3) treating the product of step (2) with hydrogen under catalytic conditions to form the compound of Formula I and I & II wherein B is ##STR6## (II.) and where it is desired to prepare compounds of Formula I wherein B is ##STR7## additionally carrying out the following steps on the products prepared by the procedures in (I.) above:(1) alkylating the lactim carbonyl by treating it with trialkyloxonium tetrafluoroborate to form the corresponding alkyl iminium ether, i.e., the compound of Formula I where B is as above and R.sup.4 =OR.sup.5 ;(2) treating the product of step (1) with an amine of formula HNR.sup.6 R.sup.7 followed by treatment with a mineral acid to form the compound of Formula I where B is as above and R.sup.4 =NR.sup.6 R.sup.7 ;(III.) and where it is desired to prepare compounds of Formula I wherein A is --CH.dbd.CH--, additionally carrying out the following steps on the products prepared by the procedures in (I.) above:(1) treating the 1,2 saturated compound with lithium diisopropyl amide to form the corresponding enolate;(2) treating the enolate of step (1) in situ with diphenyldisulfide to form the corresponding .alpha.-phenylthio compound;(3) oxidizing the product of step (2) to form the corresponding sulfoxide compound; and(4) heating the product of step (3) to form the compound of Formula I wherein A is --CH.dbd.CH--.
摘要翻译：制备下式化合物的方法：其中式（I）还可以具有部分式（III）的结构; 其中，A为（1）CH 2 CH 2; （2）CHCH; R图像是氢或甲基; R“是氢或β-甲基; R“'是β-甲基或羟基; Z是（1）氧代; （2）β-氢和α-羟基; 或（3）（Y）n Q其中n = 0或1，Y为1至12个碳原子的直链或支链烃链，Q为（a）其中R8为（4）（5）其中虚线键代替17α氢; （6）氰基; 或（7）四唑基;

3. 发明授权

US4097490A Pyroglutamic acid salts of t-butylamino-2,3-dihydroxypropane 失效
标题翻译：叔丁基氨基-2,3-二羟基丙烷的焦谷氨酸盐
公开(公告)号：US4097490A
公开(公告)日：1978-06-27
申请号：US767183
申请日：1977-02-09
申请人： Donald F. Reinhold
发明人： Donald F. Reinhold
IPC分类号： C07D207/28
摘要： Process for resolving enantiomers of 1-t-butylamino-2,3-dihydroxypropane using a pyroglutamic acid or a tartaric acid as resolving agent. The enantiomers of 1-t-butylamino-2,3-dihydroxypropane are useful in preparing .beta.-adrenergic blocking agents.
摘要翻译：使用焦谷氨酸或酒石酸作为拆分剂拆分1-叔丁基氨基-2,3-二羟基丙烷的对映异构体的方法。 1-叔丁基氨基-2,3-二羟基丙烷的对映异构体可用于制备β-肾上腺素能阻断剂。

4. 发明授权

US3692651A Process for preparing cis 5-fluoro-2-methyl - 1 - (p-methylsulfinylbenzylidene)-3-indenyl acetic acid 失效
标题翻译：制备CIS 5-氟-2-甲基-1-（对甲氧基苯乙烯基）-3-茚基乙酸的方法
公开(公告)号：US3692651A
公开(公告)日：1972-09-19
申请号：US3692651D
申请日：1970-05-01
申请人： MEYER SLETZINGER , RONALD HARMETZ , DONALD F REINHOLD , MERCK & CO INC
发明人： SLETZINGER MEYER , HARMETZ RONALD , REINHOLD DONALD F
IPC分类号： A61K31/19 , C07C45/00 , C07C45/38 , C07C45/46 , C07C45/51 , C07C47/238 , C07C47/55 , C07C49/697 , C07C57/58 , C07C57/60 , C07C57/62 , C07C59/64 , C07C59/72 , C07C59/74 , C07C59/88 , C07C205/12 , C07C209/36 , C07C317/00 , C07D295/185 , C07D303/38 , C07D309/12 , C07D331/02 , C07F3/00 , C07F3/02 , C07F9/54 , C09B23/04 , C07C147/14
CPC分类号： C07D295/185 , A61K31/19 , C07C57/62 , C07C209/365 , C07C315/04 , C07C2602/08 , C07D303/38 , C07D309/12 , C07D331/02 , C07F3/00 , C07F3/02 , C07F9/54 , C07F9/5407 , C09B23/04 , Y10S204/90 , C07C317/44 , C07C51/08
摘要： ISOMERIZATION OF TRANS 5-FLUORO-2-METHYL-1-(P-METHYLSULFINYLBENZYLIDENE)-3-INDENYL ACETIC ACID TO ITS CIS ISOMER.

5. 发明授权

US4716246A Process for L-dopa 失效
标题翻译： L-多巴的方法
公开(公告)号：US4716246A
公开(公告)日：1987-12-29
申请号：US899283
申请日：1986-08-22
申请人： Donald F. Reinhold , Torleif Utne , Newton L. Abramson
发明人： Donald F. Reinhold , Torleif Utne , Newton L. Abramson
IPC分类号： C07C227/24 , C07C227/12 , C07C229/34 , C07C229/36 , C07C99/08
CPC分类号： C07C229/36 , C07C227/24 , C07C227/34
摘要： A process for the preparation of (S)- or L-3-(3,4-dihydroxyphenyl)alanine (L-dopa) is described. The process utilizes water as reaction process solvent and proceeds via formation of an intermediate which can be kinetically resolved in a polar solvent to a precursor of the desired isomer and in which the undesired isomer can be efficiently racemized for reuse.

6. 发明授权

US4092314A Preparation of 4,6-diamino-5-arylazopyrimidines and adenine compounds 失效
标题翻译：制备4,6-二氨基-5-芳基氮嘧啶和腺嘌呤化合物
公开(公告)号：US4092314A
公开(公告)日：1978-05-30
申请号：US733489
申请日：1976-10-18
申请人： Michael C. Vander Zwan , Donald F. Reinhold
发明人： Michael C. Vander Zwan , Donald F. Reinhold
IPC分类号： C07D239/50 , C07D473/34
CPC分类号： C07D473/34 , C07D239/50
摘要： The present invention relates to a novel and useful process for preparing 4,6-diamino-5-arylazopyrimidine from an arylazomalononitrile in the presence of ammonium chloride and formamide. If desired, the 4,6-diamino-5-arylazopyrimidine may then be hydrogenated to form 4,5,6-triaminopyrimidine which, when the hydrogenation is carried out in the presence of formic acid or its derivative, gives adenine.
摘要翻译：本发明涉及一种在氯化铵和甲酰胺存在下由芳基氮杂壬腈制备4,6-二氨基-5-芳基氮嘧啶的新颖有用的方法。如果需要，可以将4,6-二氨基-5-芳基氮基嘧啶氢化形成4,5,6-三氨基嘧啶，当在甲酸或其衍生物存在下进行氢化时，得到腺嘌呤。

7. 发明授权

US3950411A Processes for asymmetric conversion of 3-fluoro-L-alanine and 2-deutero-3-fluoro-L-alanine to their D-isomers 失效
标题翻译： 3-氟-L-丙氨酸和2-氘-3-氟-L-丙氨酸不对称转化为其D-异构体的方法
公开(公告)号：US3950411A
公开(公告)日：1976-04-13
申请号：US552474
申请日：1975-02-24
申请人： Donald F. Reinhold
发明人： Donald F. Reinhold
IPC分类号： C07C53/21 , C07C59/19 , C07C99/00
CPC分类号： C07C265/00 , C07C53/21 , C07C59/19
摘要： 3-Fluoro-L-alanine is transformed by asymmetric conversion, via an intermediate L-2-(halo)-3-fluoropropionic acid, to 3-fluoro-D-alanine. The 3-fluoro-D-alanine thus obtained is a potent antibacterial agent.
摘要翻译：通过不对称转化，通过中间体L-2-（卤代）-3-氟丙酸将3-氟-L-丙氨酸转化为3-氟-D-丙氨酸。由此获得的3-氟-D-丙氨酸是有效的抗菌剂。

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