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.

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;

公开(公告)号：US4329469A

公开(公告)日：1982-05-11

申请号：US209814

申请日：1980-11-24

申请人： Torleif Utne ,  Ronald B. Jobson

发明人： Torleif Utne ,  Ronald B. Jobson

IPC分类号： C07D211/70

CPC分类号： C07D211/70

摘要： An optically impure diastereomeric salt is purified by treating a suspension of the salt in an appropriate solvent or solvent mixture with the required amount of the desired, optically pure, acid or base.

摘要翻译： 通过在合适的溶剂或溶剂混合物中用所需量的所需光学纯的酸或碱处理盐的悬浮液来纯化光学上不纯的非对映体盐。

公开(公告)号：US3992459A

公开(公告)日：1976-11-16

申请号：US571165

申请日：1975-05-01

申请人： Torleif Utne ,  Ronald B. Jobson ,  Alfred V. Lovell

发明人： Torleif Utne ,  Ronald B. Jobson ,  Alfred V. Lovell

IPC分类号： C07C51/15 ,  C07C25/18

CPC分类号： C07C51/15

摘要： Biaryl coupling, particularly to form 2,4-difluorobiphenyl, is accomplished by diazotizing an aniline and coupling the benzenediazonium salt with a second aromatic component in the presence of a strong acid, an inert finely divided solid and copper powder or a copper salt.

摘要翻译： 特别是用于形成2,4-二氟联苯的双芳基偶合是通过在强酸，惰性细分固体和铜粉或铜盐存在下，使苯胺重氮化和偶联苯二胺盐与第二芳族组分来实现的。